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5-HT Receptor Agonist

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621

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

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Isotope-Labeled Compounds

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Targets Recommended: 5-HT Receptor

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-B1473A

Serotonin Maximum Cited Publications 31 Publications Verification 5-Hydroxytryptamine; 5-HT	5-HT Receptor COMT Endogenous Metabolite	Neurological Disease
Serotonin is a monoamine neurotransmitter in the CNS and an endogenous **5-HT receptor** agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

HY-B1473

Serotonin hydrochloride Maximum Cited Publications 31 Publications Verification 5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride	5-HT Receptor COMT Endogenous Metabolite	Neurological Disease
Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous **5-HT receptor** agonist, with blood-brain barrier permeability. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

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_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor	Neurological Disease Metabolic Disease
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-B1473AS

Serotonin-d4 5-Hydroxytryptamine-d₄; 5-HT-d₄	Isotope-Labeled Compounds 5-HT Receptor COMT Endogenous Metabolite	Neurological Disease
Serotonin-d₄ is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.

HY-14151

Prucalopride 4 Publications Verification	5-HT Receptor Apoptosis Autophagy	Neurological Disease Cancer
Prucalopride is an orally active, selective and specific **5-HT 4 receptor** agonist (high affinity), with pK_is of 8.6 and 8.1 for human **5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor** signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .

HY-W015169

5-Methoxytryptamine O-Methylserotonin	Drug Metabolite 5-HT Receptor Endogenous Metabolite	Neurological Disease Cancer
5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective **5-HT receptor** agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

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_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-P1237

C-Type Natriuretic Peptide (CNP) (1-22), human 2 Publications Verification	Histamine Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
C-Type Natriuretic Peptide (CNP) (1-22), human, a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor .

HY-12694

Prucalopride succinate 4 Publications Verification R-108512	5-HT Receptor Apoptosis Autophagy	Metabolic Disease Cancer
Prucalopride succinate is an orally active, selective and specific **5-HT 4 receptor** agonist (high affinity), with pK_is of 8.6 and 8.1 for human **5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor** signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .

HY-109112

Brilaroxazine RP5063	Dopamine Receptor 5-HT Receptor	Neurological Disease Inflammation/Immunology
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .

HY-13221

BRL 54443	5-HT Receptor	Cardiovascular Disease
BRL 54443 is a potent *5-HT_1E/1F* receptor agonist (K_i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors .

HY-B1658A

Frovatriptan succinate hydrate (R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate	5-HT Receptor	Neurological Disease
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active *5-HT_1B* (pK₅₀ of 8.2) and **5-HT_1D receptor** agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for *5-HT_1B* and *5-HT_1D* over 5-HT_1A, 5-HT_1F, and 5-HT₇ and >1000-fold selectivity over other 5-HT, dopamine, histamine H₁, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .

HY-113008A

cis-Urocanic acid (Z)-Urocanic acid; cis-UCA	5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid is a **5-HT2A receptor** agonist. cis-Urocanic acid binds to **5-HT receptor with relatively high affinity (K_d*=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A* receptor .

HY-W015169A

5-Methoxytryptamine hydrochloride	5-HT Receptor Endogenous Metabolite	Neurological Disease Cancer
5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .

HY-B1473S

Serotonin-d4 hydrochloride 5-Hydroxytryptamine-d4 hydrochloride; 5-HT-d4 hydrochloride	Isotope-Labeled Compounds 5-HT Receptor Endogenous Metabolite COMT	Others
Serotonin-d₄ (5-Hydroxytryptamine-d₄) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473) . Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous **5-HT receptor** agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM .

HY-G0014A

Quetiapine sulfoxide dihydrochloride 1 Publications Verification Quetiapine S-oxide dihydrochloride	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide dihydrochloride (Quetiapine S-oxide dihydrochloride) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .

HY-153912

5-HT2A receptor agonist-3	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-3 ((S,S)-9b) is a **5-HT2A receptor** agonist with a K_i of 2.5 nM for human 5-HT2A receptor. 5-HT2A receptor agonist-3 shows 124-fold selectivity for *5-HT2A* over the structurally similar **5-HT2C receptor** .

HY-145393

5-HT2A receptor agonist-1	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-1 (Compound 3) is a selective **5-HT2A receptor** agonist with the EC₅₀ of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders .

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-P1237A

C-Type Natriuretic Peptide (CNP) (1-22), human TFA 2 Publications Verification	Histamine Receptor Endothelin Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor .

HY-124501

LY 165163 p-NH2-PE-TFMPP	5-HT Receptor	Neurological Disease
LY 165163 is a potent **5-HT presynaptic receptor** agonist. LY 165163 significantly decreases 5-HTP accumulation and increases DOPA accumulation in the cortex and striatum .

HY-16688A

RU 24969 succinate 1 Publications Verification	5-HT Receptor	Neurological Disease
RU 24969 succinate is a *5-HT* receptor agonist with K_i values of 0.38 and 2.5 nM for 5-HT_1B and 5-HT_1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease .

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_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

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-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_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-W015169S

5-Methoxytryptamine-d4 O-Methylserotonin-d₄	Isotope-Labeled Compounds 5-HT Receptor Drug Metabolite	Neurological Disease Cancer
5-Methoxytryptamine-d4 (O-Methylserotonin-d4) is the deuterium labeled 5-Methoxytryptamine (HY-W015169). 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective **5-HT receptor** agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

HY-19950

5-HT2A receptor agonist-6	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-6 (compound 47) is a selective *5-HT_2A* receptor agonist (pEC₅₀=6.58) .

HY-B0031S1

Quetiapine-d4 hemifumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₄ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-W417914

4-Methylamphetamine hydrochloride 4-MA hydrochloride	5-HT Receptor Monoamine Transporter Dopamine Receptor	Neurological Disease
4-Methylamphetamine hydrochloride is a *5-HT1A* receptor agonist that induces hypothermia in rats by binding to the *5-HT1A* receptor. Additionally, 4-Methylamphetamine hydrochloride acts on norepinephrine (NE), dopamine (DA), and serotonin (5-HT) transporters to increase the extracellular levels of these neurotransmitters. 4-Methylamphetamine hydrochloride can be used in the study of neurological disorders .

HY-116594A

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

HY-121920

25C-NBOH hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
25C-NBOH hydrochloride is a derivative of 2C-C having an N-(2-hydroxybenzyl) addition at the amine and is a potent agonist of **5-HT receptors** that shows selectivity for 5-HT2A over 5-HT2C (EC₅₀s = ~ 0.40 and 15 nM, respectively) .

HY-145841

5-HT2A receptor agonist-2	5-HT Receptor	Cardiovascular Disease
5-HT2A receptor agonist-2 is a highly potent serotonin **5-HT2 receptor** agonists. 5-HT2A receptor agonist-2 inspires 5-HT_2A, 5-HT_2B, and 5-HT_2C with EC₅₀ values of 1.7, 0.58, and 0.50 nM, respectively .

HY-N4157

Isopteropodine	mAChR 5-HT Receptor Bacterial	Neurological Disease
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors*. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial* activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-135096

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

HY-B0031S

Quetiapine-d4 fumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₄ (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-179063

5-HT2A receptor agonist-13	5-HT Receptor Dopamine Receptor Serotonin Transporter	Neurological Disease
5-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the **5-HT_2A receptor, with an EC₅₀ value of 416.9 nM and a K_i** value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the **5-HT_2B receptor (EC₅₀** = 120.2 nM), D2 receptor (K_i = 1298 nM), and has no activity towards the 5-HT_2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC₅₀ = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD) .

HY-B1473R

Serotonin hydrochloride (Standard) 5-Hydroxytryptamine hydrochloride (Standard); 5-HT hydrochloride (Standard)	5-HT Receptor Reference Standards COMT Endogenous Metabolite	Neurological Disease
Serotonin (5-Hydroxytryptamine) (Standard) hydrochloride is the analytical standard of Serotonin hydrochloride (HY-B1473). This product is intended for research and analytical applications. Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

HY-B1473S2

Serotonin-13C,D4 5-Hydroxytryptamine-¹³C,D₄; 5-HT-¹³C,D₄	Isotope-Labeled Compounds 5-HT Receptor COMT Endogenous Metabolite	Neurological Disease
Serotonin- ¹³C,D₄ (5-Hydroxytryptamine-13C,D₄) is a ¹³C- and deuterated labeled Serotonin (HY-B1473A). Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM .

HY-175657

5-HT2A receptor agonist-12	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-12 (compound 161-2) is a potent *5-HT2A* agonist with an EC₅₀ value of <100 nM for h5-HT2A .

HY-G0014

Quetiapine sulfoxide Quetiapine S-oxide	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .

HY-124296

2C-TFM hydrochloride	5-HT Receptor	Neurological Disease
2C-TFM hydrochloride is a ,5-dimethoxyphenethylamines compound with a para-trifluoromethyl substitution. 2C-TFM hydrochloride is a potent agonist of the **5-HT receptor** subtypes 5-HT2A and 5-HT2C .

HY-165624

LY-41	Drug Derivative 5-HT Receptor	Neurological Disease
LY-41 is a 2-aminotetralin (HY-W022362) derivative related to 8-OH-DPAT (HY-112061). LY-41 decreases 5-HT synthesis. LY-41 induces 5-HT motor syndrome. (R)-LY-41 and (S)-LY-41 are novel 5-HT_1A receptor agonists .

HY-114678

LY302148	5-HT Receptor	Neurological Disease
LY302148 is a receptor ligand for *5-HT_1F. Compared to the E_max of 5-HT, LY302148 behaves as a partial agonist* for the *5-HT_1F* receptor. In the [ ³⁵S]GTPγS binding assay targeting human *5-HT_1F* receptors, LY302148 exhibits good potency with an EC₅₀ value of 5.23 nM. LY302148 can be used in the research of migraine .

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-106605

Flumezapine LY 120363	Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT *receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor* agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .

HY-169786

5-HT2A receptor agonist-5	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-5 (compound I-3) is a potent *5-HT2A* receptor agonist with a K_i value of 0.017 µM. 5-HT2A receptor agonist-5 shows antidepressant activity .

HY-153091

BMY 14802	Adrenergic Receptor 5-HT Receptor Sigma Receptor	Neurological Disease
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at *serotonin (5-HT) 1A* and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .

HY-172978

5-HT2A receptor agonist-8	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-8 (compound 8) is a potent **5-HT2A receptor** agonist with an EC₅₀ of 0.6784 nM. 5-HT2A receptor agonist-8 can be used in the study of depressive disorders and bipolar disorders .

HY-172980

5-HT2A receptor agonist-9	5-HT Receptor	Neurological Disease
5-HT2A receptor agonist-9 (Compound 9) is a β-arrestin-biased **5-HT_2A receptor** agonist. 5-HT2A receptor agonist-9 can be used in the research of neurological diseases such as antidepressant and psychedelic .

Art. -Nr.	Produktname	Type

HY-100993

α-Methylserotonin maleate	Biochemical Assay Reagents
α-Methylserotonin maleate is a potent and selective agonist of **5-HT₂ receptor*. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor*-mediated phosphoinositide hydrolysis .

HY-139201E

Poly-D-lysine hydrobromide (MW 150000-300000)

PDLHB (MW 150000-300000)

Biochemical Assay Reagents

Poly-D-lysine hydrobromide (MW 150000-300000) is a synthetic polymer composed of D-lysine residues and is one of the most widely used matrices in neural cell culture applications. Poly-D-lysine hydrobromide (MW 150000-300000) can be used as a non-specific cell adhesion enhancer. Poly-D-lysine hydrobromide (MW 30000-70000) is an orally active CaSR agonist peptide that indirectly activates the 5-HT₃ receptor signaling pathway, delaying gastric emptying and thereby slowing the rate at which glucose enters the small intestine and is absorbed .

HY-15401A

WAY 163909 (hydrochloride)

Biochemical Assay Reagents

WAY 163909 hydrochloride is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 hydrochloride exhibits an EC₅₀ of 8 nM and a K_i of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 hydrochloride induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 hydrochloride alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 hydrochloride can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia .

Art. -Nr.	Produktname	Target	Research Area

HY-P1237

C-Type Natriuretic Peptide (CNP) (1-22), human 2 Publications Verification	Histamine Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
C-Type Natriuretic Peptide (CNP) (1-22), human, a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor .

HY-P1237A

C-Type Natriuretic Peptide (CNP) (1-22), human TFA 2 Publications Verification	Histamine Receptor Endothelin Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease
C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor .

HY-110366

WAY-181187 oxalate SAX-187 oxalate	5-HT Receptor	Neurological Disease
WAY-181187 (SAX-187) oxalate is a potent and selective full *5-HT6* receptor agonist with a K_i of 2.2 nM and an EC₅₀ of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-B1473A

Serotonin Maximum Cited Publications 31 Publications Verification 5-Hydroxytryptamine; 5-HT	Alkaloids Structural Classification Endogenous metabolite Indole Alkaloids	5-HT Receptor COMT Endogenous Metabolite
Serotonin is a monoamine neurotransmitter in the CNS and an endogenous **5-HT receptor** agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

HY-B1473

Serotonin hydrochloride Maximum Cited Publications 31 Publications Verification 5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride	Alkaloids Structural Classification Endogenous metabolite Indole Alkaloids Source Classification	5-HT Receptor COMT Endogenous Metabolite
Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous **5-HT receptor** agonist, with blood-brain barrier permeability. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Microorganisms Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

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-17038

Agomelatine 5+ Cited Publications S-20098	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-W015169

5-Methoxytryptamine O-Methylserotonin	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Indole Alkaloids Source Classification Cancer	Drug Metabolite 5-HT Receptor Endogenous Metabolite
5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective **5-HT receptor** agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

HY-B0229

Zolmitriptan BW-311C90; 311C90	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Indole Alkaloids Source Classification	5-HT Receptor Endogenous Metabolite
Zolmitriptan (BW-311C90; 311C90) is a **5-HT1B/1D receptor** partial agonist that can cross the blood-brain barrier, with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine .

HY-N0247

Saikosaponin B1 2 Publications Verification	Structural Classification Classification of Application Fields Umbelliferae Plants Disease Research Fields Saccharides Monosaccharides Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification Cancer	Hedgehog Smo STAT Interleukin Related TNF Receptor
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the **5-HT_2C receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer** activities thus can be studies in research for cancers such as Medulloblastoma (MB) .

HY-W015169A

5-Methoxytryptamine hydrochloride	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Indole Alkaloids Source Classification Cancer	5-HT Receptor Endogenous Metabolite
5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .

HY-N3398

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

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-N2125

Parishin C	Structural Classification Gastrodia elata Bl. Orchidaceae Phenols Plants Source Classification	5-HT Receptor iGluR Caspase Interleukin Related TNF Receptor SOD NF-κB
Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a *5-HT1A* receptor agonist with an EC₅₀ of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis .

HY-N4157

Isopteropodine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	mAChR 5-HT Receptor Bacterial
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors*. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial* activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-B1473R

Serotonin hydrochloride (Standard) 5-Hydroxytryptamine hydrochloride (Standard); 5-HT hydrochloride (Standard)	Alkaloids Structural Classification Endogenous metabolite Indole Alkaloids Source Classification	5-HT Receptor Reference Standards COMT Endogenous Metabolite
Serotonin (5-Hydroxytryptamine) (Standard) hydrochloride is the analytical standard of Serotonin hydrochloride (HY-B1473). This product is intended for research and analytical applications. Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

HY-17038A

Agomelatine hydrochloride 5+ Cited Publications S-20098 hydrochloride	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-N8200

Cassiaside B2	Monophenols Classification of Application Fields Phenols Caesalpiniaceae Cassia obtusifolia (L.) H. S. Irwin & Barneby Plants Inflammation/Immunology Disease Research Fields Source Classification	Phosphatase Monoamine Oxidase 5-HT Receptor
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a *5-HT2C* receptor agonist . ..

HY-17038B

Agomelatine (L(+)-Tartaric acid) 5+ Cited Publications S-20098 L(+)-Tartaric acid	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine L(+)-Tartaric acid is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-17038R

Agomelatine (Standard) S-20098 (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective **5-HT2C receptor antagonist with pK_i*s of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C* receptors, respectively .

HY-N4157R

Isopteropodine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	Reference Standards mAChR 5-HT Receptor Bacterial
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors*. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial* activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

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.

HY-17038AR

Agomelatine hydrochloride (Standard) S-20098 hydrochloride (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite Reference Standards
Agomelatine (hydrochloride) (Standard) is the analytical standard of Agomelatine (hydrochloride). This product is intended for research and analytical applications. Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-N0247R

Saikosaponin B1 (Standard)	Structural Classification Umbelliferae Plants Saccharides Monosaccharides Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification	Reference Standards Smo
Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the *5-HT_2C* receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .

HY-N2125R

Parishin C (Standard)	Structural Classification Gastrodia elata Bl. Orchidaceae Phenols Plants Source Classification	Reference Standards 5-HT Receptor iGluR Caspase Interleukin Related TNF Receptor SOD NF-κB
Parishin C (Standard) is the analytical standard of Parishin C (HY-N2125). This product is intended for research and analytical applications. Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a *5-HT1A* receptor agonist with an EC₅₀ of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis .

HY-W015169AR

5-Methoxytryptamine hydrochloride (Standard)	Structural Classification Alkaloids Endogenous metabolite Indole Alkaloids Source Classification	5-HT Receptor Reference Standards Endogenous Metabolite
5-Methoxytryptamine (hydrochloride) (Standard) is the analytical standard of 5-Methoxytryptamine (hydrochloride) (HY-W015169A). This product is intended for research and analytical applications. 5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .

HY-W015169R

5-Methoxytryptamine (Standard) O-Methylserotonin (Standard)	Structural Classification Alkaloids Endogenous metabolite Indole Alkaloids Source Classification	Drug Metabolite 5-HT Receptor Reference Standards Endogenous Metabolite
5-Methoxytryptamine (Standard) is the analytical standard of 5-Methoxytryptamine (HY-W015169). This product is intended for research and analytical applications. 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

HY-N2434A

(E)-[10]-Shogaol	Zingiber officinale Roscoe Structural Classification Monophenols Animals Phenols Plants Source Classification Zingiberaceae	5-HT Receptor
(E)-[10]-Shogaol is a **5-HT_1A receptor** partial agonist found in Zingiber officinale, with a K_i of 5.84 μM. (E)-[10]-Shogaol may be used in research on anxiety and depression .

Art. -Nr.	Produktname	Chemical Structure

HY-B1473AS

Serotonin-d4
Serotonin-d₄ is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.

HY-B1473S

Serotonin-d4 hydrochloride
Serotonin-d₄ (5-Hydroxytryptamine-d₄) hydrochloride is the deuterium labeled Serotonin (hydrochloride) (HY-B1473) . Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous **5-HT receptor** agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM .

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-W015169S

5-Methoxytryptamine-d4
5-Methoxytryptamine-d4 (O-Methylserotonin-d4) is the deuterium labeled 5-Methoxytryptamine (HY-W015169). 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective **5-HT receptor** agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

HY-B0031S1

Quetiapine-d4 hemifumarate
Quetiapine-d₄ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-126057S

(R)-Praziquantel-d11
(R)-Praziquantel-d₁₁ is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer .

HY-B0527AS

Amitriptyline-d6 hydrochloride

Amitriptyline-d₆ hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (K_i = 3.45 nM) and NET (K_i = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with K_i = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity.

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-B0031S

Quetiapine-d4 fumarate
Quetiapine-d₄ (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-B1473S2

Serotonin-13C,D4
Serotonin- ¹³C,D₄ (5-Hydroxytryptamine-13C,D₄) is a ¹³C- and deuterated labeled Serotonin (HY-B1473A). Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM .

HY-14546S

Aripiprazole-d8

Aripiprazole-d₈ (OPC-14597-d₈) is the deuterium labeled Aripiprazole (HY-14546). Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

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-B0716S2

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

HY-A0039S1

Eletriptan-d5
Eletriptan-d₅ is the deuterium labeled Eletriptan . Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine .

HY-17038S2

Agomelatine-d3
Agomelatine-d₃ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-14546S1

Aripiprazole-d8-1 Maximum Cited Publications 11 Publications Verification
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-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-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-B0229S

Zolmitriptan-d6
Zolmitriptan-d₆ is deuterium labeled Zolmitriptan. Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with K_is of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine .

HY-15394S

(Rac)-Rotigotine-d7 (hydrochloride)

(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (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 Kis 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-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-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-17038S1

Agomelatine-d4
Agomelatine-d₄ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-15296S1

Cabergoline-d6
Cabergoline-d₆ is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).

HY-17637S2

Lumateperone-d4

Lumateperone-d₄ (ITI-007-d₄) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .

HY-B0197AS

Naratriptan-d3 hydrochloride

Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

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-113008AS

cis-Urocanic acid-13C3
cis-Urocanic acid- ¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .

HY-G0014S

Quetiapine Sulfoxide-d8
Quetiapine Sulfoxide-d₈ is the deuterium labeled Quetiapine sulfoxide. Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .

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-106605S

Flumezapine-d8 hydrochloride

Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

HY-B1658BS

Frovatriptan-d3 succinate

Frovatriptan-d₃ (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .

HY-B0121BS1

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

HY-W742404

Bopindolol-d9

Bopindolol-d₉ ((±)-Bopindolol-d₉) is the deuterium labeled Bopindolol (HY-B1562). Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.

HY-B0121BS

Sumatriptan-d6 succinate 1 Publications Verification
Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active **5-HT1 receptor** agonist with K_is of 17 nM, 27 nM and 100 nM for *5-HT1D, 5-HT1B* and **5-HT1A receptors**, respectively. Sumatriptan succinate can be used for migraine headache research .

HY-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-14153AS

Tegaserod-13C,d3 maleate
Tegaserod- ¹³C,d₃ (maleate) is the ¹³C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract .

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-B0716S1

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

HY-A0039S

Eletriptan-d3
Eletriptan-d₃ is the deuterium labeled Eletriptan hydrobromide. Eletriptan hydrobromide is a selective 5-HT1B and 5-HT1D receptor agonist with K_i of 0.92 nM and 3.14 nM, respectively .

HY-32329S

Setiptiline-d3

Setiptiline-d₃ is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-B0121BS2

Sumatriptan-d5
Sumatriptan-d₅ is deuterated labeled Sumatriptan (HY-B0121B). Sumatriptan (GR 43175) is an orally active **5-HT1 receptor** agonist with IC₅₀s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT_1D, 5-HT_1B and 5-HT_1F receptors, respectively. Sumatriptan can be used for migraine headache research .

Art. -Nr.	Produktname		Classification

HY-172995

RS130-180		Alkynes
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT_2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .

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