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Isoforms Recommended:	5-HT₁ Receptor

Results for "

5-HT1A receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (220) Adenylate Cyclase (1) Adrenergic Receptor (28) Apoptosis (1) Bacterial (4) Biochemical Assay Reagents (1) Calcium Channel (1) Cannabinoid Receptor (1) Dopamine Receptor (77) Drug Metabolite (1) GABA Receptor (1) Histamine Receptor (3) iGluR (1) Isotope-Labeled Compounds (13) Monoamine Oxidase (1) Parasite (1) Phosphodiesterase (PDE) (1) Reactive Oxygen Species (5) Serotonin Transporter (12) Sigma Receptor (3) Wnt (1)
By Research Areas:	Cancer (18) Cardiovascular Disease (7) Endocrinology (19) Infection (3) Inflammation/Immunology (9) Metabolic Disease (4) Neurological Disease (205)

By Targets:

5-HT Receptor (220)

Adenylate Cyclase (1)

Adrenergic Receptor (28)

Apoptosis (1)

Bacterial (4)

Biochemical Assay Reagents (1)

Calcium Channel (1)

Cannabinoid Receptor (1)

Dopamine Receptor (77)

Drug Metabolite (1)

GABA Receptor (1)

Histamine Receptor (3)

iGluR (1)

Isotope-Labeled Compounds (13)

Monoamine Oxidase (1)

Parasite (1)

Phosphodiesterase (PDE) (1)

Reactive Oxygen Species (5)

Serotonin Transporter (12)

Sigma Receptor (3)

Wnt (1)

By Research Areas:

Cancer (18)

Cardiovascular Disease (7)

Endocrinology (19)

Infection (3)

Inflammation/Immunology (9)

Metabolic Disease (4)

Neurological Disease (205)

234

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1115

Buspirone hydrochloride 1 Publications Verification	5-HT Receptor Reactive Oxygen Species	Neurological Disease Cancer
Buspirone hydrochloride is a **5-HT1A receptor** agonist. Buspirone hydrochloride can be used for anxiety and depression research .

HY-122422

Gepirone	5-HT Receptor	Others
Gepirone is a selective and affinitive *5-HT_1A* agonist. Gepirone binds selectively to 5-HT_1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .

HY-75502

Rotigotine 1 Publications Verification N-0923; (-)-N 0437	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the **5-HT1A receptor*, and an antagonist of the α2B-adrenergic receptor*. Rotigotine can be used for parkinson's disease (PD) research .

HY-B1115A

Buspirone 1 Publications Verification	5-HT Receptor Dopamine Receptor Reactive Oxygen Species	Neurological Disease Cancer
Buspirone is an orally active **5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant** antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research .

HY-12709

ARC 239	Adrenergic Receptor 5-HT Receptor	Neurological Disease
ARC 239 is an α2B/C-adrenergic receptor antagonist with pK_i of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits **5-HT1A receptor with a K_i** of 63.1 nM .

HY-N3398

Lauroscholtzine N-Methyllaurotetanine	5-HT Receptor	Neurological Disease
Lauroscholtzine (N-Methyllaurotetanine), a natural alkaloid, is a **5-HT1A receptor** agonist .

HY-120939

S14063	5-HT Receptor	Neurological Disease
S14063 is a potent **5-HT1A receptor** antagonist. S14063 is devoid of β-adrenoceptor blocking properties .

HY-75502R

Rotigotine (Standard)	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Rotigotine (Standard) is the analytical standard of Rotigotine. This product is intended for research and analytical applications. Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the **5-HT1A receptor*, and an antagonist of the α2B-adrenergic receptor*. Rotigotine can be used for parkinson's disease (PD) research .

HY-120396

LY 293284	5-HT Receptor	Neurological Disease
LY 293284 is a potent and selective **5-HT1A receptor** agonist. LY 293284 results in a significant drop in core temperature and consumes more food in cholestasis rat induced by bile duct resection .

HY-122422R

Gepirone (Standard)	5-HT Receptor	Others
Gepirone (Standard) is the analytical standard of Gepirone. This product is intended for research and analytical applications. Gepirone is a selective and affinitive *5-HT_1A* agonist. Gepirone binds selectively to 5-HT_1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research .

HY-B1115AR

Buspirone (Standard)	5-HT Receptor Dopamine Receptor Reactive Oxygen Species	Neurological Disease Cancer
Buspirone (Standard) is the analytical standard of Buspirone. This product is intended for research and analytical applications. Buspirone is an orally active **5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant** antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research .

HY-106617A

Etoperidone hydrochloride	5-HT Receptor Adrenergic Receptor	Neurological Disease
Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows K_d values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .

HY-108509

BMY-14802 hydrochloride BMY-14802-1; BMS 181100 hydrochloride	Sigma Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC₅₀ of 112 nM. BMY-14802 hydrochloride is also a *5-HT1A* and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects .

HY-12959A

Repinotan hydrochloride BAY x 3702	5-HT Receptor	Neurological Disease
Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active **5-HT1A receptor agonist, with K_i** values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .

HY-123704

CGS-12066 maleate	5-HT Receptor	Neurological Disease
CGS-12066 (maleate) is a 5-HT receptor agonist. CGS-12066 has agonist effect for 5-HT_1A , 5-HT_1B,5-HT_1C and 5-HT_1D with pEC₅₀ values of 6.41, 7.56, 4.05 and 7.11, respectively. CGS-12066 can be used for the research of neurological disease .

HY-100554

BMY 7378	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
BMY 7378 is a selective antagonist of α_1D-adrenoceptor (α_1D-AR). BMY 7378 binds to membranes expressing the cloned rat α_1D-AR with a >100-fold higher affinity (K_i=2 nM) than binding to either the cloned rat α_1A-AR (K_i=800 nM) or the hamster α_1B-AR (K_i=600 nM). BMY 7378 is a *5-HT_1A* receptor partial agonist .

HY-116076

S-15535	5-HT Receptor	Neurological Disease
S-15535 is a highly selective *5-HT_1A* receptor ligand. S-15535 is an antagonist of postsynaptic *5-HT_1A* receptors and an agonist of presynaptic *5-HT_1A* receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety .

HY-106964A

(Rac)-S 16924	5-HT Receptor	Neurological Disease
(Rac)-S 16924 is a partial agonist of the *5-HT1A* receptor. (Rac)-S 16924 regulates signaling through its interaction with the *5-HT1A* receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the *5-HT1A* receptor in mental disorders, especially schizophrenia .

HY-100925

Binospirone hydrochloride	Others	Others
Binospirone hydrochloride serves as an antagonist of the 5-HT1A receptor.

HY-117575A

WAY-100135 dihydrochloride	5-HT Receptor	Neurological Disease
WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic *5-HT_1A* receptor, with an IC₅₀ of 34 nM at the rat hippocampal 5-HT_1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties .

HY-120738

p-MPPI hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
p-MPPI hydrochloride is a selective **5-HT1A receptor** antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects .

HY-19417A

Wf-516	Serotonin Transporter 5-HT Receptor	Neurological Disease
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of *5-HT1A* and 5-HT2A receptors, with K_i of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.

HY-118775

LEK 8804	Others	Others
LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.

HY-B1213

Trimipramine maleate	5-HT Receptor Bacterial	Neurological Disease
Trimipramine maleate 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 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-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-B0500

Alverine citrate 1 Publications Verification NSC 35459	5-HT Receptor	Metabolic Disease
Alverine citrate is a *5-HT_1A* receptor antagonist, with an IC₅₀ of 101 nM.

HY-B0500A

Alverine	5-HT Receptor	Metabolic Disease
Alverine citrate is a *5-HT_1A* receptor antagonist, with an IC₅₀ of 101 nM.

HY-B0500B

Alverine hydrochloride	5-HT Receptor	Metabolic Disease
Alverine hydrochloride citrate is a *5-HT_1A* receptor antagonist, with an IC₅₀ of 101 nM.

HY-144764

5-HT1A antagonist 1	5-HT Receptor	Neurological Disease
5-HT1A antagonist 1 (compound 6f) is a potent and selective antagonist of **5-HT_1A receptor, with a K_i** of 35 nM. 5-HT1A antagonist 1 can be used for the research of CNS diseases .

HY-19417

Wf-516 hydrochloride	Serotonin Transporter 5-HT Receptor	Neurological Disease
Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of *5-HT1A* and 5-HT2A receptors, with K_i of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.

HY-119775

U92016A	Others	Others
U92016A is a potent and selective agonist of the 5-HT1A receptor, with activities such as high affinity binding to the 5-HT1A receptor in vitro, causing a decrease in body temperature in vivo, and high potency and high intrinsic activity as an agonist in single-cell firing studies.

HY-100166

AP521	5-HT Receptor	Neurological Disease
AP521 is an agonist of human **5-HT_1A receptor with an IC₅₀** of 94 nM.

HY-14785

Befiradol NLX-112; F13640	5-HT Receptor	Neurological Disease
Befiradol (NLX-112) is a selective *5-HT1A* receptor agonist.

HY-14785A

Befiradol hydrochloride NLX-112 hydrochloride; F 13640 hydrochloride	5-HT Receptor	Neurological Disease
Befiradol hydrochloride (NLX-112 hydrochloride) is a selective *5-HT_1A* receptor agonist.

HY-B0716

Urapidil	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Urapidil is an α1 adrenoreceptor antagonist and a **5-HT_1A receptor** agonist.

HY-100426

Osemozotan MKC242 free base	5-HT Receptor	Others
Osemozotan (MKC242 free base) acts as an agonist for the 5-HT(1A) receptor.

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-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-116309

SDZ 216-525	5-HT Receptor	Neurological Disease
SDZ 216-525 is a selective silent antagonist of *5-HT_1A* receptor .

HY-117507

U92016A hydrochloride	5-HT Receptor	Neurological Disease
U92016A hydrochloride is a potent, metabolically stable, orally acitive *5-HT1A* receptor agonist with an exceptionally high degree of intrinsic activity . U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (K_i=0.2 nM) .

HY-P1134

Galanin (1-15) (porcine, rat)	5-HT Receptor	Neurological Disease
Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the **5-HT1A receptor** in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .

HY-101609

Lesopitron dihydrochloride E4424	5-HT Receptor	Neurological Disease
Lesopitron dihydrochloride is a full and selective *5-HT_1A* receptor agonist with IC₅₀ of 125 nM in rat hippocampal membranes.

HY-14261

Vilazodone Hydrochloride 4 Publications Verification EMD 68843 Hydrochloride; SB659746A Hydrochloride	5-HT Receptor Serotonin Transporter	Neurological Disease
Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and *5-HT_1A* receptor partial agonist.

HY-10349

WAY-100635 5+ Cited Publications	5-HT Receptor Dopamine Receptor	Neurological Disease
WAY-100635 is a potent and selective 5-HT_1A Receptor antagonist with a pIC₅₀ of 8.87, an apparent pA₂ of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 has pIC₅₀ values for *5-HT1A* and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D₄ receptor agonist .

HY-B1213R

Trimipramine maleate (Standard)	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-116594A

OPC-14523 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
OPC-14523 hydrochloride is an orally active sigma and **5-HT1A receptor** agonist, with high affinity for sigma receptors (σ1/2 IC₅₀=47/56 nM), the 5-HT1A receptor (IC₅₀=2.3 nM), and the 5-HT transporter (IC₅₀=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .

HY-106430

Piclozotan SUN N4057	5-HT Receptor	Neurological Disease
Piclozotan (SUN N4057) is a **5HT1A receptor** agonist. Piclozotan improves motor complications in Parkinson's disease model .

HY-100290

5-HT1A modulator 1	5-HT Receptor	Neurological Disease
5-HT1A modulator 1 displays very high affinities for the *5HT_1A, adrenergic α₁* and dopamine D₂ receptor with IC₅₀s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.

HY-19863

F-15599 2 Publications Verification NLX-101	5-HT Receptor	Neurological Disease
F-15599 is a highly selective G-protein biased **5-HT1A receptor agonist, with K_i** of 3.4 nM.

Cat. No.	Product Name	Target	Research Area

HY-P1134

Galanin (1-15) (porcine, rat)	5-HT Receptor	Neurological Disease
Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the **5-HT1A receptor** in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2411

Geissoschizine methyl ether	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Structural Classification Source classification Rubiaceae Plants Indole Alkaloids	5-HT Receptor
Geissoschizine methyl ether, a major indole alkaloid found in Uncaria hook, is a major active component of Yokukansan with psychotropic effects. Geissoschizine methyl ether is potent **5-HT_1A receptor** agonist .

HY-N0096

Rotundine (-)-Tetrahydropalmatine; L-Tetrahydropalmatine	Alkaloids Structural Classification Corydalis yanhusuo W. T. Wang Source classification Plants Isoquinoline Alkaloids Papaveraceae	5-HT Receptor Dopamine Receptor
Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC₅₀s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of *5-HT_1A* with an IC₅₀ of 370 nM.

HY-N0049

Nuciferine 5 Publications Verification	Structural Classification Alkaloids Aporphine Alkaloids other families Source classification Plants Isoquinoline Alkaloids	Parasite 5-HT Receptor Dopamine Receptor
Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at *5-HT_1A* (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-N3398

Lauroscholtzine N-Methyllaurotetanine	Structural Classification Alkaloids Thalictrum revolutum DC. Source classification Ranunculaceae Plants Isoquinoline Alkaloids	5-HT Receptor
Lauroscholtzine (N-Methyllaurotetanine), a natural alkaloid, is a **5-HT1A receptor** agonist .

HY-N0049R

Nuciferine (Standard)	Structural Classification Alkaloids other families Source classification Plants	5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at *5-HT_1A* (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

Cat. No.	Product Name	Chemical Structure

HY-B0716S1

Urapidil-d3
Urapidil-d₃ is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.

HY-14261S

Vilazodone-d8
Vilazodone-d₈ is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.

HY-14763S

Cariprazine-d6
Cariprazine-d₆ is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].

HY-14763S1

Cariprazine-d8
Cariprazine-d₈ is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).

HY-14546S1

Aripiprazole (1,1,2,2,3,3,4,4-d8) 5+ Cited Publications
Aripiprazole (1,1,2,2,3,3,4,4-d₈) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM[1][2].

HY-15780S

Brexpiprazole-d8
Brexpiprazole-d₈ is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].

HY-B0716S2

Urapidil-d4
Urapidil-d₄ is the deuterium labeled Urapidil[1]. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist[2].

HY-B1115S1

Buspirone-d8 (di(hydrochloride))
Buspirone-d8 dihydrochloride is the deuterium labeled Buspirone hydrochloride (HY-B1115). Buspirone hydrochloride is a **5-HT1A receptor** agonist. Buspirone hydrochloride can be used for anxiety and depression research .

HY-A0095S

Flibanserin-d4
Flibanserin-d₄ is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].

HY-B0982S

Pindolol-d7
Pindolol-d₇ (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33 nM)[1][2].

HY-A0095S1

Flibanserin-d4-1

Flibanserin-d₄-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].

HY-B1213S

Trimipramine-d3 maleate
Trimipramine-d₃ (maleate) is the deuterium labeled Trimipramine maleate. Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively[1][2].

HY-B0121BS

Sumatriptan-d6 succinate
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with K_is of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and **5-HT1A receptors**, respectively. Sumatriptan succinate can be used for migraine headache research .

HY-B0031S3

Quetiapine-d8 hemifumarate

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[1].

HY-B0031S4

Quetiapine hemifumarate-d8

Quetiapine (hemifumarate)-d₈ is the deuterium labeled Quetiapine hemifumarate[1]. 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[2].

HY-B0031S5

Quetiapine-d4-1 fumarate

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 pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B0032AS

Lurasidone-d8
Lurasidone-d₈ is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

HY-14262S1

Vilazodone-d8 hydrochloride
Vilazodone-d₈ hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial **5-HT₁A receptor** agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .

HY-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine 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[1][2][3].

HY-15780S1

Brexpiprazole-d8-1

Brexpiprazole-d₈-1 is the deuterium labeled Brexpiprazole[1]. 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)[2][3].

HY-15414AS

Vortioxetine-d8 hydrobromide
Vortioxetine-d₈ (Lu AA 21004-d₈) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414S

Vortioxetine-d8
Vortioxetine-d₈ (Lu AA 21004-d₈) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414S1

Vortioxetine-d6
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a **5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM) .**

HY-B1658BS

Frovatriptan-d3 succinate

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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