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Isoforms Recommended:	5-HT₁ Receptor mLAG-3

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human 5-HT1A receptor

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By Targets:	5-HT Receptor (51) Adenylate Cyclase (1) Adrenergic Receptor (8) Akt (1) Apoptosis (1) Bacterial (4) DNA/RNA Synthesis (1) Dopamine Receptor (28) Drug Derivative (1) Drug Metabolite (3) ERK (1) G protein-coupled Bile Acid Receptor 1 (1) HCN Channel (2) Histamine Receptor (1) Isotope-Labeled Compounds (11) JNK (1) Phytohormone (1) PKC (1) Reactive Oxygen Species (ROS) (1) Reference Standards (9) Serotonin Transporter (4) Trk Receptor (1)
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Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14544

Quetiapine 3 Publications Verification ICI204636	5-HT Receptor Dopamine Receptor	Neurological Disease
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-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-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-B0031

Quetiapine hemifumarate 3 Publications Verification	5-HT Receptor Dopamine Receptor	Neurological Disease
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-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-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-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-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-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-15780S1

Brexpiprazole-d8-1 OPC-34712-d₈-1	Isotope-Labeled Compounds Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Brexpiprazole-d₈-1 (OPC-34712-d₈-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human *5-HT1A* and dopamine 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-14544R

Quetiapine (Standard) ICI204636 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine (Standard) is the analytical standard of Quetiapine. This product is intended for research and analytical applications. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, *HT1A, 5-HT2A, 5-HT2C receptor* with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B0031R

Quetiapine hemifumarate (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human **5-HT1A receptor*. Quetiapine hemifumarate is a dopamine receptor* antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, *HT1A, 5-HT2A, 5-HT2C receptor* with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

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-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-15780R

Brexpiprazole (Standard) OPC-34712 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human *5-HT1A* and dopamine 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-15780S

Brexpiprazole-d8 OPC-34712-d₈	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
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-135555

5-Carboxamidotryptamine 5-CT	5-HT Receptor	Neurological Disease
5-Carboxamidotryptamine (5-CT) is a 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_5A, 5-HT₇ receptor agonist . 5-Carboxamidotryptamine has a K_i value of 4.6 nM for cloned human 5-HT_5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice .

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-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-100166

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

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-14546S1

Aripiprazole-d8-1 10+ Cited Publications OPC-14597-d₈	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
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 K_i of 4.2 nM .

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-133152S

Brexpiprazole S-oxide-d8 DM-3411 d₈	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
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-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-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-B0031S2

Quetiapine-d8 fumarate	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₈ (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

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-12959

Repinotan BAY x 3702 free base	5-HT Receptor	Neurological Disease
Repinotan (BAY x 3702 free base) 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 has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects .

HY-34763

7-Hydroxycarbostyril 7-Hydroxyquinolinone; 2,7-Dihydroxyquinoline	Drug Derivative	Others
7-Hydroxycarbostyril (7-Hydroxy-2(1H)-quinolinone) (Compound 7) is a quinolinone derivative. 7-Hydroxycarbostyril can be used for synthesis of Brexpiprazole (HY-15780). Brexpiprazole, a typical orally active antipsychotic agent, is a partial agonist of human *5-HT1A* and dopamine D2L receptor .

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-B1213AR

Trimipramine (Standard)	Reference Standards 5-HT Receptor Bacterial	Neurological Disease
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .

HY-B1213R

Trimipramine maleate (Standard)	Reference Standards 5-HT Receptor Bacterial	Neurological Disease
Trimipramine (maleate) (Standard) is the analytical standard of Trimipramine (maleate). This product is intended for research and analytical applications. Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .

HY-100820R

Sarizotan (Standard) EMD 128130 (Standard)	Reference Standards 5-HT Receptor Dopamine Receptor	Neurological Disease
Sarizotan (Standard) is the analytical standard of Sarizotan. This product is intended for research and analytical applications. Sarizotan (EMD 128130) is an orally active serotonin **5-HT_1A receptor** and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC₅₀ values of 6.5 nM (rat 5-HT_1A), 0.1 nM (human 5-HT_1A), 15.1 nM (rat D₂), 17 nM (human D₂), 6.8 nM (human D₃) and 2.4 nM (human D_4.2), respectively .

HY-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-119389

RGH-1756	Dopamine Receptor 5-HT Receptor	Neurological Disease
RGH-1756 is an atypical antipsychotic that has a strong and selective antagonist activity on human D₃ and less pronounced activity on human D_2L and **5HT_1A receptors** .

HY-116908

SB-272183	5-HT Receptor	Neurological Disease
SB-272183 is a selective *5-HT_1A, 5-HT_1B* and 5-HT_1D receptor antagonist. In addition, SB-272183 is also a potent and selective ligand for *5-HT_1A, 5-HT_1B* and 5-HT_1D receptors in human recombinant and native tissues with pK_i values of 8.0, 8.1 and 8.7, respectively. SB-272183 can be used in antidepressant research .

HY-B0031S3

Quetiapine-d8 hemifumarate	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₈ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B0031S4

Quetiapine hemifumarate-d8	Dopamine Receptor 5-HT Receptor	Neurological Disease
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	Dopamine Receptor 5-HT Receptor Isotope-Labeled Compounds	Neurological Disease
Quetiapine-d₄-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human **5-HT1A receptor*. Quetiapine hemifumarate is a dopamine receptor* antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, *HT1A, 5-HT2A, 5-HT2C receptor* with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-14544AS

Quetiapine-d4 hydrochloride ICI204636-d4 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Quetiapine-d₄ (hydrochloride) (ICI204636-d₄ (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, *HT1A, 5-HT2A, 5-HT2C receptor* with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

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-101225

8 Hydroxy PIPAT oxalate	5-HT Receptor Histamine Receptor	Inflammation/Immunology
8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that promotes the release of histamine from enteric mast cells. 8 Hydroxy PIPAT oxalate activates serotonergic signaling pathways, leading to the degranulation of mast cells in both guinea pig and human intestinal preparations. 8 Hydroxy PIPAT oxalate enhances the spontaneous release of histamine, which may contribute to the regulation of gastrointestinal functions. 8 Hydroxy PIPAT oxalate has potential implications for understanding and treating functional gastrointestinal disorders such as irritable bowel syndrome.

HY-100057

BMY 28674 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215	5-HT Receptor Drug Metabolite Dopamine Receptor	Neurological Disease
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype *5-HT1A* in the rat hippocampus and dorsal raphe (EC₅₀s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC₅₀s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.

HY-N9418R

Gibberellin A5 (Standard)	Phytohormone Reference Standards	Others
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .

HY-100656AS

Desmethyl cariprazine-d8	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Desmethyl cariprazine-d₈ is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC₅₀ of 8.90 at human D2 receptors, a pEC₅₀ of 8.09 at D3 receptors, and a pEC₅₀ of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca ²⁺ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

HY-100658S

Didesmethyl cariprazine-d8	Isotope-Labeled Compounds 5-HT Receptor Dopamine Receptor	Neurological Disease
Didesmethyl cariprazine-d₈ is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (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.

HY-100658R

Didesmethyl cariprazine (Standard)	5-HT Receptor Reference Standards Dopamine Receptor	Neurological Disease
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N9418R

Gibberellin A5 (Standard)	Rosaceae Plants Rosa canina Gremli ex Christ Source Classification	Phytohormone Reference Standards
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .

Cat. No.	Product Name	Chemical Structure

HY-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-14546S1

Aripiprazole-d8-1 10+ 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 K_i of 4.2 nM .

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-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-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-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-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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