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5-HT1A Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (73) Adenylate Cyclase (2) Adrenergic Receptor (7) Akt (3) Apoptosis (1) Bacterial (4) Calcium Channel (1) Cytochrome P450 (6) Dopamine Receptor (19) Drug Derivative (2) Drug Isomer (2) Drug Metabolite (3) ERK (3) GABA Receptor (1) GSK-3 (1) HCN Channel (2) Isotope-Labeled Compounds (13) JNK (3) Monoamine Oxidase (1) Phytohormone (1) PKC (3) Reactive Oxygen Species (ROS) (1) Reference Standards (11) Serotonin Transporter (21) Trk Receptor (3) Wnt (2)
By Research Areas:	Cancer (8) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (71)

By Targets:

5-HT Receptor (73)

Adenylate Cyclase (2)

Adrenergic Receptor (7)

Akt (3)

Apoptosis (1)

Bacterial (4)

Calcium Channel (1)

Cytochrome P450 (6)

Dopamine Receptor (19)

Drug Derivative (2)

Drug Isomer (2)

Drug Metabolite (3)

ERK (3)

GABA Receptor (1)

GSK-3 (1)

HCN Channel (2)

Isotope-Labeled Compounds (13)

JNK (3)

Monoamine Oxidase (1)

Phytohormone (1)

PKC (3)

Reactive Oxygen Species (ROS) (1)

Reference Standards (11)

Serotonin Transporter (21)

Trk Receptor (3)

Wnt (2)

By Research Areas:

Cancer (8)

Cardiovascular Disease (1)

Infection (1)

Inflammation/Immunology (1)

Metabolic Disease (1)

Neurological Disease (71)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Serpin

Cat. No.	상품명	Target	연구분야	Chemical Structure

HY-15414

Vortioxetine Maximum Cited Publications 10 Publications Verification Lu AA 21004	5-HT Receptor Serotonin Transporter	Infection Neurological Disease Cancer
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-14262

Vilazodone 5+ Cited Publications EMD 68843; SB659746A	5-HT Receptor Serotonin Transporter	Neurological Disease
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-14261

Vilazodone Hydrochloride 5+ Cited Publications 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-B1371

Spiperone 2 Publications Verification Spiroperidol	Dopamine Receptor 5-HT Receptor Wnt	Neurological Disease
Spiperone (Spiroperidol) is a potent dopamine D2, serotonin *5-HT_1A, and serotonin 5-HT_2A* antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases .

HY-15414A

Vortioxetine hydrobromide Maximum Cited Publications 10 Publications Verification Lu AA21004 hydrobromide	5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Lu AA 21004) hydrobromide 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-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-W052508

Norquetiapine 1 Publications Verification N-Desalkylquetiapine	Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter	Neurological Disease
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-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-124591

TC-2153	5-HT Receptor Monoamine Oxidase	Neurological Disease
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and **5-HT1A receptor*s mRNA level in midbrain. TC-2153 also inhibits* 5-HT2A receptor-mediated signaling .

HY-B0383

Almotriptan malate PNU180638	5-HT Receptor	Neurological Disease
Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine .

HY-10351A

Robalzotan hydrochloride NAD-299 hydrochloride	5-HT Receptor	Neurological Disease
Robalzotan hydrochloride (NAD-299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system .

HY-14604

Xaliproden hydrochloride 1 Publications Verification SR57746A; SR57746 hydrochloride	5-HT Receptor Dopamine Receptor Trk Receptor PKC ERK Akt JNK	Neurological Disease Metabolic Disease
Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective *5-HT1A* receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ ³⁵S]GTPγS labeling in rat brain structures rich in *5-HT1A* receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .

HY-B2169

Melperone	5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450	Neurological Disease
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone 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 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 is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly .

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-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-B0383A

Almotriptan PNU180638 free base	5-HT Receptor	Neurological Disease
Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine .

HY-100769

Hypidone hydrochloride 2 Publications Verification YL0919	5-HT Receptor	Neurological Disease
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective **5-HT_1A receptor agonist (K_i*=0.19 nM). Hypidone hydrochloride inhibits* the uptake of [ ³H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC₅₀s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .

HY-N16471

Escholtzine	5-HT Receptor Cytochrome P450	Neurological Disease
Escholtzine is an Alkaloid. Escholtzine can be isolated from Eschscholzia californica. Escholtzine is a CYP3A4 inhibitor, *5-HT_1A* receptor inhibitor with a CYP3A4 IC₅₀ of 13.4 μM, 5-HT_1A EC₅₀ of 11 μM. Escholtzine can be used for the research of anxiety, depression .

HY-19946

Eptapirone F 11440	5-HT Receptor	Neurological Disease
Eptapirone (F11440) is a potent, selective and orally active *5-HT_1A* receptor agonist (pK_i = 8.33). Eptapirone can inhibit cAMP production. Eptapirone can reduce 5-HT levels and increase corticosterone levels. Eptapirone shows potent anxiolytic and antidepressant potential. Eptapirone can be used for the research of neurological disease, such as anxiety and depression .

HY-15414R

Vortioxetine (Standard) Lu AA 21004 (Standard)	Reference Standards 5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. 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 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-111419

DSP-1053	Serotonin Transporter 5-HT Receptor	Neurological Disease
DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a K_i of 1.02 nM. DSP-1053 shows partial 5-HT_1A receptor agonistic activity with a K_i of 5.05 nM. DSP-1053 has antidepressant activity .

HY-W052508S

Norquetiapine-d8 N-Desalkylquetiapine-d₈	Isotope-Labeled Compounds	Others Neurological Disease Inflammation/Immunology
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-15414AR

Vortioxetine hydrobromide (Standard) Lu AA21004 hydrobromide (Standard)	5-HT Receptor Serotonin Transporter Reference Standards	Neurological Disease Cancer
Vortioxetine (hydrobromide) (Standard) is the analytical standard of Vortioxetine (hydrobromide). This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .

HY-15414S

Vortioxetine-d8 Lu AA 21004 d₈	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
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-W040555

Norquetiapine dihydrochloride 1 Publications Verification N-Desalkylquetiapine dihydrochloride	Drug Metabolite 5-HT Receptor HCN Channel Serotonin Transporter	Neurological Disease
Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine dihydrochloride 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 dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation .

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-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-14261S

Vilazodone-d8 1 Publications Verification	5-HT Receptor Serotonin Transporter	Neurological Disease
Vilazodone-d₈ is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.

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-10351

Robalzotan NAD-299	5-HT Receptor	Neurological Disease
Robalzotan (NAD-299) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan increases the firing rate of 5-HT cells. Robalzotan induces 5-HT1A receptor occupancy. Robalzotan has the potential for the research of a cholinergic deficit in the central -nervous system .

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-167238

RS-30199	5-HT Receptor	Neurological Disease
RS-30199 is an anxiogenic agent. RS-30199 interacts with the **5-HT_1A receptor*. RS-30199 prolongs intromission latency. RS-30199 fully inhibits* the facilitation of sexual behaviour caused by Delequamine (HY-106874) .

HY-14262S1

Vilazodone-d8 hydrochloride EMD 68843-d8; SB659746A-d8	5-HT Receptor Serotonin Transporter Isotope-Labeled Compounds	Neurological Disease
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-W052508R

Norquetiapine (Standard) N-Desalkylquetiapine (Standard)	5-HT Receptor Reference Standards	Neurological Disease
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .

HY-15414AS

Vortioxetine-d8 hydrobromide Lu AA21004-d8 hydrobromide	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
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-103109

Melperone hydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450	Neurological Disease
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-B2169S2

Melperone-d4 hydrochloride	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor Adrenergic Receptor Cytochrome P450	Neurological Disease
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-121562

SB 714786	5-HT Receptor	Neurological Disease
SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.

HY-165624A

(S)-LY-41	Drug Isomer Drug Derivative 5-HT Receptor	Neurological Disease
(S)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (S)-LY-41 is a potent and selective 5-HT1A receptor agonist. (S)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (S)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (S)-LY-41 can induce the 5-HT behavioral syndrome. (S)-LY-41can be used for the research of neurological disease, such as depression and anxiety .

HY-165624B

(R)-LY-41	Drug Isomer Drug Derivative 5-HT Receptor	Neurological Disease
(R)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (R)-LY-41 is a potent and selective 5-HT1A receptor agonist. (R)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (R)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (R)-LY-41 can induce the 5-HT behavioral syndrome but is weaker than (S)-LY-41 (HY-165624A). (R)-LY-41 can be used for the research of neurological disease, such as depression and anxiety .

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-174146

5-HT1A agonist 1	5-HT Receptor	Neurological Disease
5-HT1A agonist 1 (Compound Ex.37) is a highly selective **5-HT_1a receptor agonist (EC₅₀*=0.18 nM). 5-HT1A* agonist 1 mimicks serotonin binding to the receptor, promotes postsynaptic membrane hyperpolarization, inhibits neuronal hyperexcitability, and reduces the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is promising for research of neuropsychiatric diseases .

HY-118775

LEK 8804	5-HT Receptor	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-111985

Revospirone BAY Vq 7813	5-HT Receptor Adenylate Cyclase	Others
Revospirone (BAY Vq 7813) is a partial agonist of the *5-HT_1A* receptor with a K_i of 2 nmol/L. Revospirone inhibits adenylate cyclase activity with an IC₅₀ of 124 nmol/L .

HY-14261R

Vilazodone Hydrochloride (Standard) EMD 68843 Hydrochloride (Standard); SB659746A Hydrochloride (Standard)	Reference Standards 5-HT Receptor Serotonin Transporter	Neurological Disease
Vilazodone (Hydrochloride) (Standard) is the analytical standard of Vilazodone (Hydrochloride). This product is intended for research and analytical applications. Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and *5-HT_1A* receptor partial agonist.

HY-111419A

DSP-1053 benzenesulfonate	Serotonin Transporter 5-HT Receptor	Neurological Disease
DSP-1053, a benzylpiperidine derivative, is a potent serotonin transporter (SERT) inhibitor with a K_i of 1.02 nM. DSP-1053 shows partial *5-HT_1A* receptor agonistic activity with a K_i of 5.05 nM. DSP-1053 has antidepressant activity .

HY-106904

Nexopamil	Calcium Channel 5-HT Receptor Dopamine Receptor	Cardiovascular Disease
Nexopamil is a calcium antagonist of Ca ²⁺ channel, 5HT₂, *5HT_1A, 5HT_1C* and dopamine D₂ receptors. Nexopamil exhibits vasodilatory, cardioprotective, and platelet aggregation inhibiting effects. Nexopamil can be used for researches of stable or unstable angina and possibly of peripheral arterial occlusive disease .

HY-12709R

ARC 239 (Standard)	Adrenergic Receptor 5-HT Receptor	Neurological Disease
ARC 239 (Standard) is the analytical standard of ARC 239. This product is intended for research and analytical applications. ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM .

HY-110024A

S-14506	5-HT Receptor	Neurological Disease
S-14506 hydrochloride is a potent *5-HT1A* agonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent .

HY-19946A

Eptapirone fumarate F 11440 fumarate	5-HT Receptor	Neurological Disease
Eptapirone fumarate (F11440 fumarate) is a potent, selective and orally active *5-HT_1A* receptor agonist (pK_i = 8.33). Eptapirone fumarate can inhibit cAMP production. Eptapirone fumarate can reduce 5-HT levels and increase corticosterone levels. Eptapirone fumarate shows potent anxiolytic and antidepressant potential. Eptapirone fumarate can be used for the research of neurological disease, such as anxiety and depression .

Cat. No.	상품명	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-N16471

Escholtzine	Eschscholzia californica Chamisso Structural Classification Alkaloids Other Alkaloids Plants Papaveraceae Source Classification	5-HT Receptor Cytochrome P450
Escholtzine is an Alkaloid. Escholtzine can be isolated from Eschscholzia californica. Escholtzine is a CYP3A4 inhibitor, *5-HT_1A* receptor inhibitor with a CYP3A4 IC₅₀ of 13.4 μM, 5-HT_1A EC₅₀ of 11 μM. Escholtzine can be used for the research of anxiety, depression .

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.	상품명	Chemical Structure

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-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-14261S

Vilazodone-d8 1 Publications Verification
Vilazodone-d₈ is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.

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-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-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-B0383AS

Almotriptan hydrochloride-d6

Almotriptan-d₆ (PNU180638-d₆) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

HY-B0383AS2

Almotriptan-d3 benzoate

Almotriptan-d₃ benzoate (PNU180638 free base-d₃) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.

HY-143797S

Almotriptan-d6 maleate

Almotriptan-d₆ (PNU180638-d₆) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.

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.

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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