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5-HT1A receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (175) Adenylate Cyclase (1) Adrenergic Receptor (40) Apoptosis (2) Bacterial (5) Biochemical Assay Reagents (1) Calcium Channel (1) Cytochrome P450 (4) Dopamine Receptor (80) Drug Isomer (1) Drug Metabolite (5) HCN Channel (2) Histamine Receptor (3) iGluR (1) Isotope-Labeled Compounds (23) Parasite (1) Phosphodiesterase (PDE) (1) Phytohormone (1) Reactive Oxygen Species (ROS) (3) Reference Standards (37) Serotonin Transporter (13) Sigma Receptor (2) Wnt (2)
By Research Areas:	Cancer (17) Cardiovascular Disease (9) Endocrinology (14) Infection (2) Inflammation/Immunology (6) Metabolic Disease (7) Neurological Disease (160)

By Targets:

5-HT Receptor (175)

Adenylate Cyclase (1)

Adrenergic Receptor (40)

Apoptosis (2)

Bacterial (5)

Biochemical Assay Reagents (1)

Calcium Channel (1)

Cytochrome P450 (4)

Dopamine Receptor (80)

Drug Isomer (1)

Drug Metabolite (5)

HCN Channel (2)

Histamine Receptor (3)

iGluR (1)

Isotope-Labeled Compounds (23)

Parasite (1)

Phosphodiesterase (PDE) (1)

Phytohormone (1)

Reactive Oxygen Species (ROS) (3)

Reference Standards (37)

Serotonin Transporter (13)

Sigma Receptor (2)

Wnt (2)

By Research Areas:

Cancer (17)

Cardiovascular Disease (9)

Endocrinology (14)

Infection (2)

Inflammation/Immunology (6)

Metabolic Disease (7)

Neurological Disease (160)

185

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15780

Brexpiprazole 5+ Cited Publications OPC-34712	5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human *5-HT1A* and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM) .

HY-B1115A

Buspirone 3 Publications Verification	5-HT Receptor Dopamine Receptor Reactive Oxygen Species (ROS)	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-B1517

Alprenolol 5+ Cited Publications (RS)-Alprenolol; dl-Alprenolol	5-HT Receptor	Cardiovascular Disease Cancer
Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of *5-HT1A* and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .

HY-10349

WAY-100635 Maximum Cited Publications 12 Publications Verification	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-B0032A

Lurasidone 10+ Cited Publications SM-13496	5-HT Receptor Dopamine Receptor	Neurological Disease
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-HT_1A* receptor with an IC₅₀ of 6.75 nM.

HY-B1517A

Alprenolol hydrochloride 5+ Cited Publications (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride	5-HT Receptor	Cardiovascular Disease Cancer
Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of *5-HT1A* and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .

HY-75502

Rotigotine 3 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-A0095

Flibanserin 2 Publications Verification BIMT-17; BIMT-17BS	5-HT Receptor	Neurological Disease Cancer
Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin **5-HT1A receptor** agonist and 5-HT2A receptor antagonist with K_i values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research ^- .

HY-N0096

Rotundine (-)-Tetrahydropalmatine; L-Tetrahydropalmatine	5-HT Receptor Dopamine Receptor	Neurological Disease
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-10349A

WAY-100635 maleate Maximum Cited Publications 12 Publications Verification	5-HT Receptor Dopamine Receptor	Neurological Disease
WAY-100635 maleate 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 maleate has pIC₅₀ values for *5-HT1A* and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D₄ receptor agonist .

HY-B0032

Lurasidone Hydrochloride 10+ Cited Publications SM-13496 Hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of *5-HT_1A* receptor with an IC₅₀ of 6.75 nM.

HY-103152

GR 113808 5+ Cited Publications	5-HT Receptor	Neurological Disease Inflammation/Immunology
GR 113808 is a potent and highly selective *5-HT₄ receptor* antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors .

HY-17407

Ziprasidone hydrochloride monohydrate 3 Publications Verification CP 88059 hydrochloride monohydrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and *5-HT_1A* (K_i=3.4 nM) .

HY-A0007

Rotigotine Hydrochloride 3 Publications Verification N-0923 Hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the **5-HT1A receptor*, and an antagonist* of the α2B-adrenergic receptor, with K_i of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-14542A

Ziprasidone hydrochloride 3 Publications Verification CP-88059 hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and *5-HT_1A* (K_i=3.4 nM) .

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-19818A

NAN-190 hydrobromide	5-HT Receptor	Neurological Disease
NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of *5-HT_1A* .

HY-B0716

Urapidil	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
Urapidil is an α1 adrenoreceptor antagonist and a **5-HT_1A receptor** agonist that can cross the blood-brain barrier .

HY-103415

Nemonapride YM-09151-2; Emonapride	Dopamine Receptor 5-HT Receptor	Neurological Disease
Nemonapride is a highly potent dopamine D₂ receptor antagonist with a K_i of 0.06 nM. Nemonapride also activates **5-HT_1A receptor with an IC₅₀** of 34 nM. Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals .

HY-100658

Didesmethyl cariprazine	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-HT_1A* receptor, and antagonist at the human 5-HT_2B receptor (K_i: 1.41 nM (human D_2L), 0.056 nM (human D₃), 1.7 nM (human 5-HT_1A), 0.52 nM (human 5-HT_2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .

HY-B0731A

Perospirone SM-9018 free base	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT_2A receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of *5-HT_1A* receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-B0731

Perospirone hydrochloride SM-9018	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT_2A receptor (K_i of 0.6 nM) and dopamine D₂ receptor (K_i of 1.4 nM). Perospirone hydrochloride is also a partial agonist of *5-HT_1A* receptor (K_i of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-19686

Ipsapirone TVX Q 7821 free base	5-HT Receptor	Neurological Disease
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a *5-HT_1A* receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits *5-HT_1A* receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT₂ and the α₁-adrenergic function .

HY-15394

(Rac)-Rotigotine hydrochloride N-0437 hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the **5-HT1A receptor*, and an antagonist* of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-W795507

Cyanopindolol	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for *5-HT1A* and 5-HT1B receptor (K_i: 2.1 and 3 nM respectively) .

HY-G0002

Lurasidone metabolite 14326	Drug Metabolite Dopamine Receptor 5-HT Receptor	Neurological Disease
Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 can be used in the research of schizophrenia and bipolar depression .

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-14782

Adoprazine SLV313	5-HT Receptor Dopamine Receptor	Neurological Disease
Adoprazine (SLV313) is a full **5-HT_1A receptor** agonist with a pEC₅₀ of 9 at cloned h5-HT_1A receptors. Adoprazine (SLV313) is a full D₂ and D₃ receptor antagonist with pA₂s of 9.3 and 8.9 at hD₂ and hD₃ receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics .

HY-133152

Brexpiprazole S-oxide DM-3411	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide (DM-3411) 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-HT_1A* and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT_2A receptor antagonist with a K_i of 0.47 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-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-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-B0716S2

Urapidil-d4	Isotope-Labeled Compounds Adrenergic Receptor 5-HT Receptor	Endocrinology
Urapidil-d₄ is the deuterium labeled Urapidil . Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist .

HY-19742A

Lecozotan hydrochloride SRA-333 hydrochloride	5-HT Receptor	Neurological Disease
Lecozotan (SRA-333) hydrochloride is an orally active and selective antagonist of *5-HT_1A* with a K_i of 4.5 nM for cloned human 5-HT_1A receptor. Lecozotan hydrochloride enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. Lecozotan hydrochloride has the potential for mild-to-moderate Alzheimer's disease (AD) research .

HY-15780A

Brexpiprazole hydrochloride OPC-34712 hydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human *5-HT1A* and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM) .

HY-B1517AR

Alprenolol hydrochloride (Standard) (RS)-Alprenolol hydrochloride (Standard); dl-Alprenolol hydrochloride (Standard)	Reference Standards 5-HT Receptor	Cancer
Alprenolol (hydrochloride) (Standard) is the analytical standard of Alprenolol (hydrochloride). This product is intended for research and analytical applications. Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of *5-HT1A* and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .

HY-12709

ARC 239 1 Publications Verification	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-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-12701A

U-99194 maleate U-99194A; PNU-99194A maleate; JPC-211 maleate	Dopamine Receptor	Neurological Disease
U-99194 (PNU-99194) maleate is a selective, potent dopamine D3 receptor antagonist (K_i =160 nM). U-99194 maleate inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 maleate abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 maleate significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 maleate can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors .

HY-101322A

MM 77 dihydrochloride	5-HT Receptor	Neurological Disease
MM 77 dihydrochloride is a potent postsynaptic antagonist of the **5-HT_1A receptor**. MM 77 dihydrochloride exhibits anxiolytic-like activity .

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-106943

1192U90	Dopamine Receptor 5-HT Receptor	Neurological Disease
1192U90 is an antipsychotic agent, dopamine D₂ receptor antagonist as well as serotonin 5-HT_1a receptor agonist. 1192U90 reduces the number of spontaneously firing neurons in the limbic dopamine system .

HY-105328

S-14489	5-HT Receptor	Neurological Disease
S-14489 is an orally active selective postsynaptic **5-HT1A receptor** antagonist with a pK_i of 9.2. S-14489 can act as a 5-HT1A autoreceptor agonist and inhibit striatal 5-hydroxytryptophan accumulation. S-14489 can be used for the research of neurological disease .

HY-B1517B

Alprenolol benzoate	5-HT Receptor	Cardiovascular Disease Cancer
Alprenolol benzoate is an orally active non-selective β-adrenoceptor antagonist and an antagonist of *5-HT1A* and 5-HT1B receptors. Alprenolol benzoate is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent .

HY-B0716R

Urapidil (Standard)	Reference Standards 5-HT Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Urapidil (Standard) is the analytical standard of Urapidil. This product is intended for research and analytical applications. Urapidil is an α1 adrenoreceptor antagonist and a **5-HT_1A receptor** agonist that can cross the blood-brain barrier .

HY-19372

SSR-181507 hydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
SSR-181507 hydrochloride is a dopamine D₂ receptor antagonist and *5-HT_1A* receptor agonist. SSR-181507 antagonizes Apomorphine (HY-12723)-induced climbing in mice and stereotypies in rats. SSR-181507 hydrochloride can be used in the research of depression and anxiety .

HY-B1115AR

Buspirone (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor Reactive Oxygen Species (ROS)	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-A0095B

Flibanserin hydrochloride BIMT-17 hydrochloride; BIMT-17BS hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Flibanserin hydrochloride (BIMT-17 hydrochloride) is an orally active *5-HT_1A* receptor agonist and 5-HT_2A receptor antagonist with binding affinities K_i of 1 nM and 49 nM, respectively. Flibanserin hydrochloride also binds to dopamine D4 receptors with a K_i of 4-24 nM. Flibanserin hydrochloride has antidepressant and anxiolytic effects and can be used in the study of hypoactive sexual desire disorder (HSDD) .

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-A0007S

Rotigotine-d7 hydrochloride N-0923 D7 Hydrochloride	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Rotigotine-d₇ (N-0923-d₇) hydrochloride is the deuterium labeled Rotigotine(HY-75502). 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.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0049

Nuciferine 5+ Cited Publications	Alkaloids Aporphine Alkaloids other families Plants Isoquinoline Alkaloids Source Classification	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-N0096

Rotundine (-)-Tetrahydropalmatine; L-Tetrahydropalmatine	Alkaloids Corydalis yanhusuo W. T. Wang Plants Isoquinoline Alkaloids Papaveraceae Source Classification	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-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 .

HY-N0049R

Nuciferine (Standard)	Alkaloids other families Plants Source Classification	Reference Standards 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-15780S1

Brexpiprazole-d8-1

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 D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM) .

HY-15780S

Brexpiprazole-d8

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 D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM) ^.

HY-W052508S

Norquetiapine-d8

Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .

HY-B0716S2

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

HY-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ (DM-3411 D₈) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). 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 K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 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-A0007S

Rotigotine-d7 hydrochloride

Rotigotine-d₇ (N-0923-d₇) hydrochloride is the deuterium labeled Rotigotine(HY-75502). 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-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-B0031S2

Quetiapine-d8 fumarate

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-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-B2169S2

Melperone-d4 hydrochloride

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-B0716S1

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

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) .

HY-15394S1

(Rac)-Rotigotine-d3 hydrochloride

(Rac)-Rotigotine-d₃ hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

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 .

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) .

HY-W654010

Lurasidone-d8-1 hydrochloride
Lurasidone-d₈-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of *5-HT_1A* receptor with an IC₅₀ of 6.75 nM .

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 .

HY-B0731AS

Perospirone-d8

Perospirone-d₈ (SM-9018-d₈ (free base)) is deuterium labeled Perospirone. Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT_2A receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of 5-HT_1A receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .

HY-B0031S4

Quetiapine hemifumarate-d8

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 .

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-14544AS

Quetiapine-d4 hydrochloride

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

HY-15414S2

Vortioxetine-d4
Vortioxetine-d₄ (Lu AA 21004-d₄) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A 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-HT1A agonist and a partial agonist of 5-HT1B (K_i: 15 nM, 33 nM) .

HY-15414S3

Vortioxetine-d3
Vortioxetine-d₃ (Lu AA 21004-d₃) is a deuterium labeled Vortioxetine (HY-15414). 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-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-100658S

Didesmethyl cariprazine-d8

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 (K_i: 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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