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human serotonin receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (28) Serotonin Transporter (7) Adrenergic Receptor (1) Apoptosis (4) Bacterial (4) CDK (1) Checkpoint Kinase (Chk) (1) Dopamine Receptor (7) Dopamine Transporter (2) Drug Metabolite (1) Histamine Receptor (6) Isotope-Labeled Compounds (2) mAChR (2) Monoamine Transporter (1) nAChR (1) p38 MAPK (1) PARP (1) Phytohormone (1) Reference Standards (6) SARS-CoV (1) Sodium Channel (1) Trk Receptor (1)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Inflammation/Immunology (4) Metabolic Disease (4) Neurological Disease (27)

By Targets:

5-HT Receptor (28)

Serotonin Transporter (7)

Adrenergic Receptor (1)

Apoptosis (4)

Bacterial (4)

CDK (1)

Checkpoint Kinase (Chk) (1)

Dopamine Receptor (7)

Dopamine Transporter (2)

Drug Metabolite (1)

Histamine Receptor (6)

Isotope-Labeled Compounds (2)

mAChR (2)

Monoamine Transporter (1)

nAChR (1)

p38 MAPK (1)

PARP (1)

Phytohormone (1)

Reference Standards (6)

SARS-CoV (1)

Sodium Channel (1)

Trk Receptor (1)

By Research Areas:

Cancer (4)

Cardiovascular Disease (1)

Inflammation/Immunology (4)

Metabolic Disease (4)

Neurological Disease (27)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor Serotonin Transporter

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1213

Trimipramine maleate 1 Publications Verification	5-HT Receptor Bacterial	Neurological Disease
Trimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, 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-14153

Tegaserod 4 Publications Verification	5-HT Receptor Apoptosis	Metabolic Disease Cancer
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-14153A

Tegaserod maleate 4 Publications Verification SDZ-HTF-919; HTF-919	5-HT Receptor Apoptosis	Neurological Disease Metabolic Disease Cancer
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod maleate has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-B1165

Cyproheptadine (hydrochloride sesquihydrate) 3 Publications Verification	p38 MAPK Checkpoint Kinase (Chk) Histamine Receptor 5-HT Receptor CDK PARP Apoptosis	Cancer
Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia .

HY-100656

Desmethyl cariprazine	Dopamine Receptor 5-HT Receptor	Neurological Disease
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-HT_1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT_1A receptors, and suppresses serotonin-induced Ca ²⁺ release at 5-HT_2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

HY-147276

Izuforant JW1601	Histamine Receptor	Inflammation/Immunology
Izuforant (JW1601) (Compound 24) is an orally active histamine H4 receptor (H4R) antagonist with an IC₅₀ of 36 nM against human H4R. Izuforant also shows binding affinity of human serotonin 3 receptor (h5-HT3R) with an IC₅₀ of 9.1 μM. Izuforant exhibits strong anti-pruritic and anti-inflammatory efficacies .

HY-100820

Sarizotan 1 Publications Verification EMD 128130	5-HT Receptor Dopamine Receptor	Neurological Disease
Sarizotan (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively .

HY-N2411

Geissoschizine methyl ether 1 Publications Verification	5-HT Receptor	Neurological Disease
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ ³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .

HY-B0170A

Azatadine dimaleate Azatadine maleate	Histamine Receptor SARS-CoV	Inflammation/Immunology
Azatadine dimaleate (Azatadine maleate) is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis .

HY-18137

PF-04995274	5-HT Receptor	Neurological Disease
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT₄R) agonist. PF-04995274 has an EC₅₀ range of 0.26-0.47 nM for human 5-HT_4A/4B/4D/4E (K_i range of 0.15-0.46 nM), and has an EC₅₀ range of 0.59-0.65 nM for rat 5-HT_4S/4L/4E (K_i of 0.30 nM for rat 5-HT_4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .

HY-101250

Glemanserin MDL11939	Serotonin Transporter	Neurological Disease
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT_2A (K_i=2.89, 0.54 and 2.5 nM for rat 5-HT_2A, rabbit 5-HT_2A and human 5-HT_2A, respectively) .

HY-110023

Zimelidine dihydrochloride	Serotonin Transporter	Neurological Disease
Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .

HY-135096

Amitriptyline-d3 hydrochloride	Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor	Neurological Disease
Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .

HY-118796

4-Hydroxy MET 4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine	5-HT Receptor Serotonin Transporter	Neurological Disease
4-Hydroxy MET (4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine) is a synthetic tryptamine psychoactive substance. 4-Hydroxy MET is a partial 5-HT2A receptor agonist, a serotonin transporter inhibitor and weak norepinephrine transporter inhibitor. 4-Hydroxy MET affects emotional, motoric, and cognitive functions via serotonergic hallucinogenic activity .

HY-B1213A

Trimipramine	5-HT Receptor Bacterial	Neurological Disease
Trimipramine is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, 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-103115

Pruvanserin hydrochloride EMD 281014; LY 2422347 hydrochloride	5-HT Receptor	Neurological Disease
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT_2A receptor antagonist with IC₅₀ values of 0.35 nM and 1 nM for human and rat 5-HT_2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .

HY-W128798

Sulfabenz	5-HT Receptor	Neurological Disease
Sulfabenz (Compound 9) is an amine-substituted N1-phenylsulfonyl indole derivative. Sulfabenz has binding activity to human 5-HT6 serotonin receptor (K_i: 200 nM). Sulfabenz can be used to study the ligand binding mechanism of 5-HT6 receptor and 5-HT6 receptor-related neurological diseases .

HY-120464

PF-05212377 SAM-760	5-HT Receptor	Neurological Disease
PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .

HY-B0170

Azatadine	Histamine Receptor mAChR nAChR 5-HT Receptor	Inflammation/Immunology
Azatadine is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine induces sedation and exhibits topical anesthetic properties. Azatadine can be used for the research of allergic rhinitis .

HY-B1213AR

Trimipramine (Standard)	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

Trimipramine maleate (Standard)	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-130351

25H-NBOMe hydrochloride	5-HT Receptor	Neurological Disease
25H-NBOMe hydrochloride is an agonist for the rat and human serotonin 5-HT2A receptors with K_i values of 1.19 and 2.83 nM, respectively .

HY-117574

SB 207710	5-HT Receptor	Cardiovascular Disease
SB 207710 is a highly selective antagonist of the 5-HT4 receptor that has been shown to effectively block the positive inotropic effect induced by serotonin in human right atrial appendage preparations .

HY-100820B

Sarizotan dihydrochloride EMD 128130 dihydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Sarizotan dihydrochloride (EMD 128130) is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively .

HY-100820A

Sarizotan hydrochloride EMD 128130 hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Sarizotan hydrochloride is an orally active serotonin 5-HT_1A receptor and dopamine receptor agonist. Sarizotan hydrochloride (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively .

HY-100820R

Sarizotan (Standard) 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-HT_1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively .

HY-171794

AZD1134	5-HT Receptor	Neurological Disease
AZD1134 is an orally active, brain-penetrant and highly selective 5-HT₁B receptor antagonist with IC₅₀ values of 2.9 nM (human) and 0.108 nM (guinea pig), respectively. AZD1134 increases synaptic serotonin levels in guinea pigs. AZD1134 is promising for research of psychiatric disorders, such as depression and anxiety .

HY-W740014

N-Desmethyl Zolmitriptan 183C91; DZT	5-HT Receptor	Neurological Disease
N-Desmethyl Zolmitriptan (183C91; DZT) is the active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Zolmitriptan (HY-B0229). N-Desmethyl Zolmitriptan (183C91; DZT) is an agonist of 5-HT1B receptors and induces constriction in isolated human cerebral arteries (EC50=100 nM).

HY-101250R

Glemanserin (Standard) MDL11939 (Standard)	Reference Standards Serotonin Transporter	Neurological Disease
Glemanserin (Standard) is the analytical standard of Glemanserin. This product is intended for research and analytical applications. Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .

HY-14153S

Tegaserod-d11	5-HT Receptor Apoptosis Isotope-Labeled Compounds	Metabolic Disease Cancer
Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-B0170AR

Azatadine dimaleate (Standard) Azatadine maleate (Standard)	Histamine Receptor Reference Standards	Metabolic Disease Inflammation/Immunology
Azatadine dimaleate (Standard) is the analytical standard of Azatadine dimaleate. This product is intended for research and analytical applications. Azatadine dimaleate (Azatadine maleate) is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis .

HY-100057

BMY 28674 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-N9418R

Gibberellin A5 (Standard)	Phytohormone Reference Standards	Others
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-100656AS

Desmethyl cariprazine-d8	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-W680886

6-APDB	Monoamine Transporter Serotonin Transporter Dopamine Transporter 5-HT Receptor	Neurological Disease
6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT₂ family receptors. For NET, 6-APDB has an IC₅₀ of 0.56 μM and a K_i of 18 μM; for SERT, it has an IC₅₀ of 2.3 μM and a K_i of 23 μM; for DAT, it has an IC₅₀ of 33 μM and a K_i of >30 μM, and affinity for rat and mouse TAAR1, with K_i values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse .

HY-182247

D-473	Serotonin Transporter Dopamine Transporter	Neurological Disease
D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2411

Geissoschizine methyl ether 1 Publications Verification	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Structural Classification Rubiaceae Plants Indole Alkaloids Source Classification	5-HT Receptor
Geissoschizine methyl ether is an orally active, blood-brain barrier permeable alkaloid, and a partial agonist of the 5-HT₁A receptor. It can be isolated from Uncaria hook. Geissoschizine methyl ether potently inhibits the binding of [ ³H]8-OH-DPAT to the 5-HT₁A receptor in a concentration-dependent manner, with an IC₅₀ of 0.904 μM. It ameliorates isolation-induced increased aggression and reduced sociability in mice. Geissoschizine methyl ether promotes oligodendrocyte differentiation and remyelination in the medial prefrontal cortex of adult mice .

HY-N9418R

Gibberellin A5 (Standard)	Rosaceae Plants Rosa canina Gremli ex Christ Source Classification	Phytohormone Reference Standards
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 .

Cat. No.	Product Name	Chemical Structure

HY-14153S

Tegaserod-d11
Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

Tegaserod-d11

Tegaserod-d₁₁ is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a 5-HT_2B receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .

HY-100656AS

Desmethyl cariprazine-d8
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.

Desmethyl cariprazine-d8

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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