Search Result
Results for "
human D2 receptors
" in MedChemExpress (MCE) Product Catalog:
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-14544
-
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ICI204636
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
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Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
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- HY-15780
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Brexpiprazole
Maximum Cited Publications
6 Publications Verification
OPC-34712
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
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Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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-
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- HY-B0590
-
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Ro 1-9569
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Monoamine Transporter
Dopamine Receptor
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Neurological Disease
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Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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-
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- HY-B0520A
-
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Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Benztropine mesylate (Benzatropine mesylate) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
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-
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- HY-B0031
-
|
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5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
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Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
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- HY-B0590S
-
|
Ro 1-9569-d6
|
Monoamine Transporter
|
Neurological Disease
|
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Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
-
- HY-B1213
-
|
|
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy .
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- HY-32350
-
|
1α,25-Dihydroxy Vitamin D2
|
VD/VDR
Drug Metabolite
Endogenous Metabolite
|
Metabolic Disease
|
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Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid X receptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
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- HY-100656
-
|
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Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
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Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
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- HY-101348
-
|
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Dopamine Receptor
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Neurological Disease
|
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L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
|
-
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- HY-14545
-
|
(Rac)-Aramisulpride; (Rac)-Esamisulpride; DAN 2163
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Amisulpride ((Rac)-Aramisulpride) is a racemic (50:50) mixture of the R-Amisulpride (HY-109167) and S-Amisulpride (HY-126068). Amisulpride is a dopamine D2/D3 receptor antagonist with Ki values of 2.8 and 3.2 nM for human dopamine b>D2 and b>D3, respectively. Amisulpride is a 5-HT7 receptor antagonist with a Ki of 44 nM. Amisulpride can be used in psychiatric research .
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- HY-110000
-
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Dopamine Receptor
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Neurological Disease
|
|
(+)-PD 128907 hydrochloride is a selective dopamine D2/D3 receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively.
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-
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- HY-100820
-
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EMD 128130
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
|
Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
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-
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- HY-B0590A
-
|
Ro 1-9569 Racemate
|
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
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- HY-B0520
-
|
Benzatropine; Benzotropine
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Cancer
|
|
Benztropine (Benzatropine; Benzotropine) is an orally active and BBB-permeable centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
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- HY-100658
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
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-
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- HY-10847B
-
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SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
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-
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- HY-14545A
-
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(Rac)-Aramisulpride hydrochloride; (Rac)-Esamisulpride hydrochloride; (Rac)-DAN 2163 hydrochloride
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Dopamine Receptor
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Neurological Disease
|
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Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
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-
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- HY-14545S
-
|
(Rac)-Aramisulpride-d5; (Rac)-Esamisulpride-d5; DAN 2163-d5
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Dopamine Receptor
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Neurological Disease
Cancer
|
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Amisulpride-d5 is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
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- HY-116941
-
|
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Dopamine Receptor
|
Neurological Disease
|
|
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM) .
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- HY-15780S1
-
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OPC-34712-d8-1
|
Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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- HY-14544R
-
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ICI204636 (Standard)
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Reference Standards
5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
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Quetiapine (Standard) is the analytical standard of Quetiapine. This product is intended for research and analytical applications. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-B0031R
-
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Reference Standards
5-HT Receptor
Dopamine Receptor
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Neurological Disease
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Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-13213
-
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AM211 free acid
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Prostaglandin Receptor
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Inflammation/Immunology
Endocrinology
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AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
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- HY-103409
-
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Dopamine Receptor
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Neurological Disease
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ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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- HY-15780R
-
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OPC-34712 (Standard)
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Reference Standards
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
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Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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-
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- HY-15780S
-
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OPC-34712-d8
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Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
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Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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- HY-13706
-
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TM30089 Racemate
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Prostaglandin Receptor
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Endocrinology
Cancer
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CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist, with a Ki of 0.6 nM for hCRTH2, selective over human thromboxane A2 receptor TP (Ki, >10000 nM) or PGD2 receptor DP (Ki, 1200 nM). CAY10471 Racemate also has effect on mouse and rat orthologs of CRTH2 .
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- HY-177122
-
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Dopamine Receptor
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Neurological Disease
|
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Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments .
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- HY-14330
-
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Dopamine Receptor
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Neurological Disease
|
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ABT-724, a chemical probe, is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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- HY-15780A
-
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OPC-34712 hydrochloride
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
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Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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- HY-B1213A
-
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5-HT Receptor
Bacterial
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Neurological Disease
|
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Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
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- HY-B0031S2
-
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Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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-
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- HY-N3945R
-
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O,O-Dimethylisoboldine (Standard); S-(+)-Glaucine (Standard); NSC 34396 (Standard)
|
Reference Standards
Phosphodiesterase (PDE)
Calcium Channel
Adrenergic Receptor
Dopamine Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
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|
Glaucine (Standard) is the analytical standard of Glaucine. This product is intended for research and analytical applications. Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 μM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities .
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- HY-112320
-
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Dopamine Receptor
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Neurological Disease
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UCSF34 (Compound 54) is a Haloperidol (HY-14538) analogue. UCSF34 binds to the human D2L receptor, with an estimated pKi of 7.49. UCSF34 can be used in the research of schizophrenia .
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- HY-34763
-
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7-Hydroxyquinolinone; 2,7-Dihydroxyquinoline
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Drug Derivative
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Others
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7-Hydroxycarbostyril (7-Hydroxy-2(1H)-quinolinone) (Compound 7) is a quinolinone derivative. 7-Hydroxycarbostyril can be used for synthesis of Brexpiprazole (HY-15780). Brexpiprazole, a typical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor .
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- HY-W329175
-
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SKF-104557
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Dopamine Receptor
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Neurological Disease
|
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N-Despropyl Ropinirole (SKF-104557) is an active metabolite of the dopamine D2 receptor agonist Ropinirole (HY-B0623). N-Despropyl Ropinirole is a full agonist at human D2 and D3 receptors. N-Despropyl Ropinirole is a partial agonistof the hD4 receptor .
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- HY-137308
-
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15R-PGD2
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Prostaglandin Receptor
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Inflammation/Immunology
|
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15(R)-Prostaglandin D2 is a potential prostatic hormone DP(2) receptor (Prostaglandin Receptor) agonist with anti-inflammatory activity. 15(R)-Prostaglandin D2 increases actin polymerization in human eosinophils and increases cAMP levels in platelets .
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- HY-14545R
-
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(Rac)-Aramisulpride (Standard); (Rac)-Esamisulpride (Standard); DAN 2163 (Standard)
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Reference Standards
Dopamine Receptor
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Neurological Disease
Cancer
|
|
Amisulpride (Standard) is the analytical standard of Amisulpride. This product is intended for research and analytical applications. Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively.
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-
-
- HY-14545S1
-
-
-
- HY-100820B
-
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EMD 128130 dihydrochloride
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
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Sarizotan dihydrochloride (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
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- HY-100820A
-
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EMD 128130 hydrochloride
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5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
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Sarizotan hydrochloride is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan hydrochloride (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
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- HY-B0590E
-
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Ro 1-9569 mesylate
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Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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-
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- HY-B0031S3
-
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Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
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Neurological Disease
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Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-U00423
-
-
-
- HY-B0031S4
-
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Dopamine Receptor
5-HT Receptor
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Neurological Disease
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Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate . Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-B0031S5
-
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Dopamine Receptor
5-HT Receptor
Isotope-Labeled Compounds
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Neurological Disease
|
|
Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
-
- HY-100820R
-
|
EMD 128130 (Standard)
|
Reference Standards
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Sarizotan (Standard) is the analytical standard of Sarizotan. This product is intended for research and analytical applications. Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively .
|
-
-
- HY-14544AS
-
|
ICI204636-d4 hydrochloride
|
Isotope-Labeled Compounds
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
-
- HY-B0590R
-
|
Ro 1-9569 (Standard)
|
Reference Standards
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-W021008S
-
|
Dimethylhydroxyfuranone-d2
|
Isotope-Labeled Compounds
Fungal
|
Infection
|
|
Sotolone-d2 (Dimethylhydroxyfuranone-d2) is deuterated labeled Sotolone. Sotolone is an activator of the human olfactory receptor OR8D1. Sotolone activates the human olfactory receptor OR8D1, with EC50 values of 84.98 μM and 167.2 μM for its S-enantiomer and R-enantiomer, respectively. Sotolone has unique aroma profiles: (R)-sotolone exhibits smoky, burnt, herbal and grassy notes; (S)-sotolone presents sweet, milky, sour and nutty notes. Sotolone also acts as an antifungal agent, showing moderate inhibitory activity against Magnaporthe oryzae in vitro .
|
-
- HY-B0590S3
-
|
TBZ-d7-d7; Ro 1-9569-d7
|
Isotope-Labeled Compounds
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-122147
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
L-644698 is a potent and selective human recombinant prostaglandin D2 (PGD2) receptor (hDP) agonist with Ki values of 0.9, 267, 3730, 9280 nM for hDP, hEP2, hEP3, hEP4, respectively. L-644698 induces cyclic AMP production with an EC50 value of 0.5 nM .
|
-
- HY-171328
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to human D2 receptor and human D3 receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [ 35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing human D3 receptors). RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity .
|
-
- HY-32350S1
-
|
1α,25-Dihydroxy Vitamin D2-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
VD/VDR
|
Metabolic Disease
|
|
Ercalcitriol-d3 (1α,25-Dihydroxy Vitamin D2-d3) is the deuterium labeled Ercalcitriol (HY-32350). Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid X receptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
|
-
- HY-21995
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor Ki values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent .
|
-
- HY-155466
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Boc-MIF-1-Am (compound 2) is a human dopamine D2 receptor enhancer (EC50=17.82 nM) and is a bioconjugate of melanostatin (MIF-1) and amantadine. Boc-MIF-1-Am (200 μM) exhibited mild neurotoxicity in SH-SY5Y cells .
|
-
- HY-19186
-
|
CI 1007
|
Dopamine Receptor
|
Neurological Disease
|
|
PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with Ki values of 25.5 nM and 16.6 nM for human D2 and D3 receptors, respectively and lower affinity for D4.2 receptors (Ki=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology .
|
-
- HY-B0520AS1
-
|
|
Dopamine Receptor
Histamine Receptor
mAChR
|
Cancer
|
|
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
- HY-B0520AR
-
|
Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)
|
Reference Standards
Dopamine Receptor
mAChR
Histamine Receptor
|
Neurological Disease
Cancer
|
|
Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
- HY-B0520AS
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
mAChR
Histamine Receptor
|
Neurological Disease
Cancer
|
|
Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
|
-
- HY-101392S1
-
-
- HY-100057
-
|
6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215
|
5-HT Receptor
Drug Metabolite
Dopamine Receptor
|
Neurological Disease
|
|
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
|
-
- HY-123189
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guinea pigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .
|
-
- HY-101349
-
|
|
Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
|
-
- HY-101349A
-
|
|
Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
|
-
- HY-119389
-
-
- HY-14545B
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
SEP4199 is an orally active 5-HT7 receptor ligand, with a Ki value of 66 nM for human 5-HT7R and 16 nM for human D2R. SEP4199 mediates antidepressant effects. SEP4199 is applicable for the research of bipolar depression .
|
-
- HY-B1213AR
-
|
|
Reference Standards
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
|
-
- HY-B1213R
-
|
|
Reference Standards
5-HT Receptor
Bacterial
|
Neurological Disease
|
|
Trimipramine (maleate) (Standard) is the analytical standard of Trimipramine (maleate). This product is intended for research and analytical applications. Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .
|
-
- HY-101348R
-
|
|
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
L-741626 (Standard) is the analytical standard of L-741626. This product is intended for research and analytical applications. L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
|
-
- HY-111241
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
SV 293 is a selective antagonist with neutral antagonist activity. SV 293 binds to human D2 receptors with 100-fold higher affinity and has lower affinity for human D3 and D4 dopamine receptor subtypes. SV 293 was found to block the effects of the full agonist quinpirole in forskolin-dependent adenylate acylase inhibition assays and electrophysiological assays. SV 293 can be used as a useful pharmacological tool to study the role of dopamine D2-like receptor subtypes in dopamine pathways associated with neurological, neuropsychiatric and movement disorders .
|
-
- HY-W708196
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dehydrohaloperidol, Haloperidol (HY-14538) analogue, is a selective human dopamine D2 receptor antagonist with a pKd of 8 and a pki of 8. Dehydrohaloperidol can be used for the research of schizophrenia .
|
-
- HY-100656AS
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
|
-
- HY-13213A
-
-
- HY-100658S
-
|
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
|
-
- HY-100658R
-
|
|
5-HT Receptor
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
|
-
- HY-N0166S
-
|
Donaxine-d2
|
Adrenergic Receptor
Reverse Transcriptase
|
Others
|
|
Gramine-d2 is the deuterium labeled Gramine . Gramine (Donaxine) is a natural alkaloid isolated from giant reed , acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively . Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist . Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties .
|
-
- HY-103409R
-
|
|
Reference Standards
Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 trihydrochloride (Standard) is the analytical standard of ABT-724 trihydrochloride (HY-103409). This product is intended for research and analytical applications. ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
|
-
- HY-10847BR
-
|
SB-277011A hydrochloride (Standard)
|
Reference Standards
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (Standard) is the analytical standard of SB-277011 (hydrochloride) (HY-10847B). This product is intended for research and analytical applications. SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
|
-
- HY-180109
-
|
Benzo-17R-Resolvin D2
|
TNF Receptor
Interleukin Related
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Benzo-17R-RvD2 (Benzo-17R-Resolvin D2) is a benzo-containing analog of RvD2 (HY-121636). Benzo-17R-RvD2 enhances human macrophage efferocytosis, limits neutrophil infiltration, reduces TNF-α, and increases IL-1 receptor antagonist in peritonitis. Benzo-17R-RvD2 promotes E. coli killing by human leukocytes and reduces neutrophil swarm area without compromising anti-Candida activity. Benzo-17R-RvD2 activates the human-RvD2 receptor with an EC50 ∼1.5 nM. Benzo-17R-RvD2 can be used in research on inflammation-associated diseases such as cardiovascular disease, cancer, neuroinflammation, pain, and muscle regeneration .
|
-
- HY-121675A
-
|
BOL-148 D-Tartrate; Bromolysergide D-Tartrate
|
5-HT Receptor
G protein-coupled Bile Acid Receptor 1
|
Neurological Disease
|
|
2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
|
-
- HY-47412
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Cariprazine impurity 1 is a dopamine D2 receptor (D2R) agonist. Cariprazine impurity 1 modulates D2R-mediated Gi/o signaling pathway to inhibit cAMP production, and regulates D2R-mediated β-arrestin2 recruitment pathway .
|
-
- HY-183776
-
|
|
Dopamine Receptor
|
Others
|
|
Dopamine D3 receptor agonist-2 is a selective dopamine D3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamine D2 receptor (Ki= 7.67nM) .
|
-
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0590S
-
|
|
|
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
-
- HY-14545S
-
|
|
|
Amisulpride-d5 is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
|
-
-
- HY-15780S1
-
|
|
|
Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
|
-
-
- HY-15780S
-
|
|
|
Brexpiprazole-d8 (OPC-34712-d8) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
|
-
-
- HY-B0031S2
-
|
|
|
Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
-
- HY-14545S1
-
|
|
|
Amisulpride-d5 N-Oxide is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
|
-
-
- HY-B0031S3
-
|
|
|
Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
-
- HY-B0031S4
-
|
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Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate . Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-B0031S5
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Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-14544AS
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Quetiapine-d4 (hydrochloride) (ICI204636-d4 (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
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- HY-W021008S
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Sotolone-d2 (Dimethylhydroxyfuranone-d2) is deuterated labeled Sotolone. Sotolone is an activator of the human olfactory receptor OR8D1. Sotolone activates the human olfactory receptor OR8D1, with EC50 values of 84.98 μM and 167.2 μM for its S-enantiomer and R-enantiomer, respectively. Sotolone has unique aroma profiles: (R)-sotolone exhibits smoky, burnt, herbal and grassy notes; (S)-sotolone presents sweet, milky, sour and nutty notes. Sotolone also acts as an antifungal agent, showing moderate inhibitory activity against Magnaporthe oryzae in vitro .
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- HY-B0590S3
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Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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- HY-32350S1
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Ercalcitriol-d3 (1α,25-Dihydroxy Vitamin D2-d3) is the deuterium labeled Ercalcitriol (HY-32350). Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid X receptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
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- HY-B0520AS1
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Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
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- HY-B0520AS
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Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
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- HY-101392S1
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Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively) .
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- HY-100656AS
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Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
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- HY-100658S
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Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
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- HY-N0166S
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Gramine-d2 is the deuterium labeled Gramine . Gramine (Donaxine) is a natural alkaloid isolated from giant reed , acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively . Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist . Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties .
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