Search Result
Results for "
histamine H1
" in MedChemExpress (MCE) Product Catalog:
37
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-30234S
-
|
Histamine Receptor
HCV
TRP Channel
|
Cancer
|
Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .
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-
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- HY-107495
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NSC19005
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Histamine Receptor
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Inflammation/Immunology
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Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine . Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA) .
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-
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- HY-B1589A
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-
-
- HY-B0895
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-
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- HY-100280
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-
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- HY-B1303A
-
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Mebhydrolin is a specific histamine H1 receptor antagonist.
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-
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- HY-B1281
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Pyrilamine maleate
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Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
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-
-
- HY-B1303
-
-
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- HY-B2168
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-
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- HY-B0298A
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HS-592 fumarate; Meclastine fumarate
|
Histamine Receptor
|
Neurological Disease
Endocrinology
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Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
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-
-
- HY-B0298
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HS-592; Meclastine
|
Histamine Receptor
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Neurological Disease
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Clemastine (HS-592) is a potent and orally active histamine receptor H1 antagonist. Clemastine is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
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-
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- HY-U00018
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-
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- HY-101724
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NNC-05-1869 hydrochloride
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Histamine Receptor
|
Inflammation/Immunology
Endocrinology
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ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
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-
-
- HY-B0286A
-
-
-
- HY-14447
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-
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- HY-B1589AS
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-
-
- HY-B0548S1
-
-
-
- HY-B0298AR
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HS-592 fumarate (Standard); Meclastine fumarate (Standard)
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Histamine Receptor
|
Neurological Disease
Endocrinology
|
Clemastine (fumarate) (Standard) is the analytical standard of Clemastine (fumarate). This product is intended for research and analytical applications. Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects .
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-
-
- HY-B0538A
-
-
-
- HY-123829
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-
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- HY-B0814
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(R)-Cetirizine
|
|
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Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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-
-
- HY-W010841
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(R)-Cetirizine dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
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Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-105542
-
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Histamine Receptor
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Neurological Disease
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Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research .
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- HY-19489S
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-
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- HY-B1305
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-
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- HY-A0178
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AY 56012
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Isothipendyl (AY 56012), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist. Isothipendyl is a primary metabolite .
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- HY-101601
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- HY-13710A
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Dimethindene maleate is a selective histamine H1 antagonist with antihistamine effects. Dimethindene maleate can be used for the research of hypersensitivity reactions .
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- HY-17039
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R89674
|
Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .
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- HY-17428
-
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Histamine Receptor
Endogenous Metabolite
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Inflammation/Immunology
Endocrinology
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Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .
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-
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- HY-17428A
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-
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- HY-B0303A
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-
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- HY-B0298AS
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-
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- HY-B0548AS
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-
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- HY-B0303
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|
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Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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- HY-B0814S
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(R)-Cetirizine-d4(dihydrochloride)
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Isotope-Labeled Compounds
Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
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- HY-N0054
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- HY-B0524A
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- HY-B0524
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- HY-D0237
-
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Histamine Receptor
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Inflammation/Immunology
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Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist . Betahistine mesylate is used for the study of rheumatoid arthritis (RA) .
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- HY-13710
-
-
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- HY-B2168S
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-
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- HY-17428B
-
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Histamine Receptor
Endogenous Metabolite
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Inflammation/Immunology
Endocrinology
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Tripelennamine citrate, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine citrate lessens the allergic response of the organism caused by histamine. Tripelennamine citrate can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .
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-
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- HY-W010841R
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(R)-Cetirizine dihydrochloride (Standard)
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Histamine Receptor
|
Inflammation/Immunology
Endocrinology
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Levocetirizine (dihydrochloride) (Standard) is the analytical standard of Levocetirizine (dihydrochloride). This product is intended for research and analytical applications. Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-117501
-
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Histamine Receptor
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Inflammation/Immunology
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Dexchlorpheniramine is an potent and blood-brain barrier (BBB) penetrant histamine 1 (H1) receptor antagonist with anticholinergic properties. Dexchlorpheniramine can be used for researching allergies .
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-
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- HY-B0286AR
-
Chlorphenamine maleate (Standard)
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Chlorpheniramine (maleate) (Standard) is the analytical standard of Chlorpheniramine (maleate). This product is intended for research and analytical applications. Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC50 of 12 nM .
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- HY-131256
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine Impurity C is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist [1] [2] .
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- HY-131256A
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine Impurity C dihydrochloride is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist [1] [2] .
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- HY-12966
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- HY-14447S
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- HY-A0191
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(+)-Brompheniramine; (S)-Brompheniramine
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Dexbrompheniramine is an orally active H1 receptor antagonist. Dexbrompheniramine is an antihistamine that reduces the effects of natural chemical histamine. Dexbrompheniramine can be used for the research of hay fever and urticaria .
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- HY-131579
-
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Drug Metabolite
|
Inflammation/Immunology
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Deschloro Cetirizine Dihydrochloride is a Cetirizine impurity. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.
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- HY-101052
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HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 10 4 times more active than histamine in H2-mediated effects in natural suppressor cells .
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- HY-B0814S1
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(R)-Cetirizine-d4
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Isotope-Labeled Compounds
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Inflammation/Immunology
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Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-B0674
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LAS-W 090; RP64305
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
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- HY-B1808A
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- HY-107559
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Histamine Receptor
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Neurological Disease
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GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .
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- HY-101690
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- HY-17428R
-
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Histamine Receptor
Endogenous Metabolite
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Inflammation/Immunology
Endocrinology
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Tripelennamine (hydrochloride) (Standard) is the analytical standard of Tripelennamine (hydrochloride). This product is intended for research and analytical applications. Tripelennamine hydrochloride, an ethylenediamine derivative, is a potent histamine H1-receptor antagonist. Tripelennamine hydrochloride lessens the allergic response of the organism caused by histamine. Tripelennamine hydrochloride can be used for the research of rhinitis, conjunctivitis, and allergic and anaphylactic reactions .
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- HY-17043
-
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- HY-B0303AS1
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- HY-B0303AS
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- HY-Y0217
-
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Drug Metabolite
|
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N-Carbethoxy-4-piperidone is a metabolite of Loratadine (HY-17043). Loratadine is a selective inverse peripheral histamine H1-receptor agonist, and shows anti-dengue-virus (DENV) activity .
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- HY-B0548
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist.
Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder .
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- HY-B0462A
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- HY-B1301
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Triprolidine hydrochloride monohydrate, a first-generation antihistamine, is an oral active histamine H1 antagonist. Triprolidine hydrochloride monohydrate can be used for the research of allergic rhinitis. Triprolidine hydrochloride monohydrate exhibits spinal motor and sensory block in rats .
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- HY-17042
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-17042A
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P071
|
Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-B0462
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- HY-B0970
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4-Diphenylmethoxy-1-methylpiperidine hydrochloride
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Histamine Receptor
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Neurological Disease
Endocrinology
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Diphenylpyraline hydrochloride is a potent histamine H1 receptor antagonist. Diphenylpyraline hydrochloride acts as an orally active antihistamine agent with antimuscarinic and antiallergic effects. Diphenylpyraline hydrochloride can be used for the relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders in vivo.
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- HY-B0303AR
-
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Histamine Receptor
Endogenous Metabolite
Bacterial
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Inflammation/Immunology
Endocrinology
Cancer
|
Diphenhydramine (hydrochloride) (Standard) is the analytical standard of Diphenhydramine (hydrochloride). This product is intended for research and analytical applications. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
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- HY-B0548A
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
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- HY-B1317
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Neohetramine
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|
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Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases .
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- HY-162231
-
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Histamine Receptor
mAChR
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Inflammation/Immunology
|
HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases .
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- HY-100660A
-
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Drug Metabolite
|
Others
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Cetirizine Impurity B dihydrochloride is an impurity of Cetirizine dihydrochloride. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-100661
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Cetirizine Impurity D is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response .
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- HY-107431
-
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Histamine Receptor
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Inflammation/Immunology
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Diphenylpyraline is a potent histamine H1 receptor antagonist. Diphenylpyraline acts as an orally active antihistamine agent with antimuscarinic and antiallergic effects. Diphenylpyraline can be used for the research of allergic diseases, including rhinitis and hay fever, and pruritic skin disorders et.al .
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- HY-B0524AS
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- HY-12752
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Trimeprazine
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Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
|
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
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- HY-B0640A
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WAL801 hydrochloride
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
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- HY-30234A
-
-
- HY-B0640
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WAL801
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Histamine Receptor
|
Inflammation/Immunology
Endocrinology
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Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action .
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- HY-121356
-
-
- HY-108411
-
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Histamine Receptor
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Inflammation/Immunology
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Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
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- HY-A0027
-
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Histamine Receptor
Phosphodiesterase (PDE)
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Inflammation/Immunology
Endocrinology
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Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
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- HY-A0027A
-
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Histamine Receptor
Phosphodiesterase (PDE)
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Inflammation/Immunology
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases .
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- HY-17043S
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-
- HY-17043S1
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-
- HY-30234
-
-
- HY-I0021
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
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- HY-B0674S
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Ebastine-d5 is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1][2].
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- HY-B2178
-
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Histamine Receptor
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Inflammation/Immunology
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Emedastine difumarate is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
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- HY-I0021A
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
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Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus .
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- HY-17042AS
-
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Isotope-Labeled Compounds
Histamine Receptor
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Inflammation/Immunology
|
Cetirizine-d4 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-17042AS1
-
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Isotope-Labeled Compounds
Histamine Receptor
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Inflammation/Immunology
|
Cetirizine-d8 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-17042S
-
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Histamine Receptor
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Inflammation/Immunology
|
Cetirizine-d4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-12532
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R 43512
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Histamine Receptor
Potassium Channel
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Inflammation/Immunology
Endocrinology
|
Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K + channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects .
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- HY-17042S1
-
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Histamine Receptor
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Inflammation/Immunology
|
Cetirizine-d8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-B1794
-
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|
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Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects .
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- HY-A0015
-
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Histamine Receptor
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Inflammation/Immunology
Endocrinology
|
Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
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- HY-B0524AS1
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- HY-W062109
-
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Endogenous Metabolite
Histamine Receptor
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Inflammation/Immunology
|
Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis .
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- HY-101232
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ICI 125211
|
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .
|
-
- HY-B0674S1
-
-
- HY-123205
-
|
Histamine Receptor
P2X Receptor
5-HT Receptor
|
Inflammation/Immunology
|
Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca 2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin .
|
-
- HY-117046A
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .
|
-
- HY-B0548AS2
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine-d8 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
|
-
- HY-B0548AS1
-
Vistaril-d4' dihydrochloride; Atarax-d4' dihydrochloride
|
|
|
Hydroxyzine-d4 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
|
-
- HY-B0462AS
-
-
- HY-B1794A
-
|
Dopamine Receptor
Histamine Receptor
Bacterial
Amyloid-β
|
Infection
Neurological Disease
|
Thiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects .
|
-
- HY-14277A
-
R 50547 hydrochloride
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-14277
-
R 50547
|
Histamine Receptor
Neurotensin Receptor
Integrin
|
Inflammation/Immunology
|
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
|
-
- HY-A0027AS
-
|
Isotope-Labeled Compounds
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
|
-
- HY-B0725S
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
|
Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
|
-
- HY-B0548AR
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Hydroxyzine (dihydrochloride) (Standard) is the analytical standard of Hydroxyzine (dihydrochloride). This product is intended for research and analytical applications. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder .
|
-
- HY-B0164
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
|
-
- HY-B0164A
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
|
-
- HY-10791
-
-
- HY-108058A
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Immethridine dihydrobromide is a selective histamine H3 receptor (H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research .
|
-
- HY-B1193
-
-
- HY-121356S1
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
|
-
- HY-121356S
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Endocrinology
Cancer
|
Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
|
-
- HY-14328
-
PNU-101387G; U-101387G
|
Dopamine Receptor
|
Neurological Disease
|
Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively .
|
-
- HY-B0640AR
-
WAL801 hydrochloride (Standard)
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Epinastine (hydrochloride) (Standard) is the analytical standard of Epinastine (hydrochloride). This product is intended for research and analytical applications. Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action .
|
-
- HY-12394
-
Dosulepin; Dothep
|
Histamine Receptor
5-HT Receptor
|
Neurological Disease
|
Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain,idiopathic fibromyalgia syndrome or rheumatoid arthritis .
|
-
- HY-19443
-
|
Histamine Receptor
Lipoxygenase
|
Inflammation/Immunology
|
UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guinea pigs. UCB-35440 can be used for research on asthma and skin inflammation .
|
-
- HY-136587
-
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
|
-
- HY-108411S
-
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
|
Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
|
-
- HY-B0640S
-
WAL801-13C,d3 hydrobromide
|
Isotope-Labeled Compounds
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
|
-
- HY-W062109S
-
|
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
|
-
- HY-147336
-
|
Drug Metabolite
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
|
-
- HY-B0352
-
-
- HY-A0015A
-
|
Others
|
Inflammation/Immunology
Endocrinology
|
(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
|
-
- HY-103093
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo .
|
-
- HY-B0462S
-
|
Histamine Receptor
SARS-CoV
|
Infection
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
Azelastine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Azelastine hydrochloride. Azelastine- 13C,d3 (hydrochloride), an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine- 13C,d3 (hydrochloride) can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
|
-
- HY-B0157A
-
HC 20511 fumarate
|
Histamine Receptor
Endogenous Metabolite
SARS-CoV
Influenza Virus
|
Inflammation/Immunology
Endocrinology
Cancer
|
Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .
|
-
- HY-B0480
-
(±)-Brompheniramine maleate
|
Histamine Receptor
mAChR
Potassium Channel
Sodium Channel
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .
|
-
- HY-B0157
-
HC 20-511
|
|
|
Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .
|
-
- HY-B0480A
-
(±)-Brompheniramine
|
|
|
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research .
|
-
- HY-A0077S1
-
|
5-HT Receptor
Adrenergic Receptor
Apoptosis
Autophagy
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- HY-B0352S2
-
-
- HY-B0352R
-
Org3770 (Standard); 6-Azamianserin (Standard)
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Mirtazapine (Standard) is the analytical standard of Mirtazapine. This product is intended for research and analytical applications. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
|
-
- HY-B0352S3
-
-
- HY-B0725
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
|
-
- HY-107647
-
|
mAChR
Histamine Receptor
|
Inflammation/Immunology
|
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
|
-
- HY-148825
-
-
- HY-101094
-
R79598
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
|
-
- HY-B1101
-
Pimetixene
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-B1101A
-
Pimetixene maleate
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-B0725R
-
|
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
Doxepin (Hydrochloride) (Standard) is the analytical standard of Doxepin (Hydrochloride). This product is intended for research and analytical applications. Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2 . Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant .. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system .. Doxepin has also been proposed as a protective factor against oxidative stress ..
|
-
- HY-10564
-
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis .
|
-
- HY-10564S
-
MCI-9042-d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Cardiovascular Disease
|
Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
|
-
- HY-B1658A
-
(R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate
|
5-HT Receptor
|
Neurological Disease
|
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
|
-
- HY-B1658B
-
(R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate
|
5-HT Receptor
|
Neurological Disease
|
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
|
-
- HY-B1658BS
-
(R)-Frovatriptan-d3 succinate; SB 209509-d3 succinate; VML 251-d3 succinate
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
|
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
|
-
- HY-101063
-
|
|
|
Amthamine is a histamine receptor (H1R-H4R) agonist. Amthamine can produce liver congestion and necrosis of liver cells. Amthamine can be used to study the induction effect of H1R-H4 agonist on hepatotoxicity .
|
-
- HY-107565
-
|
Others
|
Inflammation/Immunology
|
2-Pyridylethylamine is a histamine-1 (H1R) receptor agonist. 2-Pyridylethylamine can reduce the joint injury induced by formalin in rats. 2-Pyridylethylamine can be used to study the spinal cord release of neuropeptide (NPY) .
|
-
- HY-111501
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R .
|
-
- HY-W014941
-
|
Histamine Receptor
|
Neurological Disease
|
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats .
|
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* This product has been "discontinued".
Optimized version of product available:
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Chemical Structure |
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- HY-30234S
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Clemizole-d4 is a deuterium labeled Clemizole. Clemizole is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication .
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- HY-B0548S1
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Hydroxyzine-d8 is deuterium labeled Hydroxyzine. Hydroxyzine is a histamine H1-receptor antagonist[1].
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- HY-19489S
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(±)-Levomepromazine-d6 is the deuterium labeled Methotrimeprazine, which is a D3 dopamine and Histamine H1 receptor antagonist.
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- HY-B1589AS
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Carbinoxamine-d6 (maleate) is the deuterium labeled Carbinoxamine maleate salt. Carbinoxamine maleate salt is a histamine H1 receptor antagonist.
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- HY-B0298AS
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Clemastine-d5 (fumarate) is the deuterium labeled Clemastine fumarate. Clemastine fumarate (HS-592 fumarate) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
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- HY-B0548AS
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Hydroxyzine-d4 (dihydrochloride) is deuterium labeled Hydroxyzine. Hydroxyzine is a heterocyclic histamine H1-receptor antagonist. Hydroxyzine has anticholinergic, anxiolytic and analgesic properties[1].
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- HY-B0814S
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Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
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- HY-B2168S
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Mequitazine-d8 hydrobromide is deuterated labeled Mequitazine (HY-B2168). Mequitazine is a potent, and long-acting histamine H1 antagonist.
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- HY-14447S
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Bilastine-d6 is the deuterium labeled Bilastine. Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria[1][2].
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- HY-B0814S1
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Levocetirizine-d4 ((R)-Cetirizine-d4) is the deuterium-labeled Levocetirizine (HY-B0814) . Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria .
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- HY-B0303AS1
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Diphenhydramine-d5 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
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- HY-B0303AS
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Diphenhydramine-d6 (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].
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- HY-B0524AS
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Betahistine-d3 (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
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- HY-17043S
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Loratadine-d4 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
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- HY-17043S1
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Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
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- HY-B0674S
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Ebastine-d5 is the deuterium labeled Ebastine. Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research[1][2].
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- HY-17042AS
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Cetirizine-d4 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-17042AS1
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Cetirizine-d8 (dihydrochloride) is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-17042S
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Cetirizine-d4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-17042S1
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Cetirizine-d8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
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- HY-B0524AS1
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Betahistine- 13C,d3 (dihydrochloride) is the 13C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
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- HY-B0674S1
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Ebastine-d6 is deuterated labeled Ebastine (HY-B0674). Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research .
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- HY-B0548AS2
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Hydroxyzine-d8 (dihydrochloride) is the deuterium labeled Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder[1][2].
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- HY-B0462AS
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Azelastine- 13C,d3 is deuterium labeled Azelastine. Azelastine, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
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- HY-A0027AS
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Fenspiride-d5 is the deuterium labeled Fenspiride. Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases[1][2][3].
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- HY-B0725S
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Doxepin-d3 (hydrochloride) is a deuterium labeled Doxepin Hydrochloride. Doxepin hydrochloride is an orally active tricyclic antidepressant. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2[1][2].
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- HY-121356S1
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Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
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- HY-121356S
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Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner[1]. Carebastine suppresses the expression of macrophage migration inhibitory factor[2].
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- HY-108411S
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Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
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- HY-B0640S
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Epinastine- 13C,d3 (hydrobromide) is the 13C- and deuterium labeled Epinastine. Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action[1][2][3][4].
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- HY-W062109S
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Olopatadine-d6 is the deuterium labeled Olopatadine[1]. Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis[2][3].
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- HY-B0462S
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Azelastine- 13C,d3 (hydrochloride) is the 13C- and deuterium labeled Azelastine hydrochloride. Azelastine- 13C,d3 (hydrochloride), an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine- 13C,d3 (hydrochloride) can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2[1][2][3][4].
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- HY-A0077S1
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Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
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- HY-B0352S2
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Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
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- HY-B0352S3
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Mirtazapine-d4 hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively .
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- HY-10564S
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Sarpogrelate-d3 (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
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- HY-B1658BS
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Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
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