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5-Hydroxytryptamine Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (31) Adrenergic Receptor (5) Apoptosis (6) Caspase (2) Cholinesterase (ChE) (1) COMT (4) COX (2) Cytochrome P450 (1) Dopamine Receptor (5) Dopamine Transporter (4) Endogenous Metabolite (4) FGFR (2) GABA Receptor (1) Histamine Receptor (4) Histone Demethylase (1) Isotope-Labeled Compounds (7) mAChR (5) Monoamine Oxidase (2) p38 MAPK (2) Potassium Channel (5) Reference Standards (5) Serotonin Transporter (9) Sodium Channel (4) TGF-β Receptor (2) Trace Amine-associated Receptor (TAAR) (1) Transthyretin (TTR) (2) Trk Receptor (4)
By Research Areas:	Cancer (8) Cardiovascular Disease (3) Endocrinology (5) Inflammation/Immunology (7) Metabolic Disease (4) Neurological Disease (29)

By Targets:

5-HT Receptor (31)

Adrenergic Receptor (5)

Apoptosis (6)

Caspase (2)

Cholinesterase (ChE) (1)

COMT (4)

COX (2)

Cytochrome P450 (1)

Dopamine Receptor (5)

Dopamine Transporter (4)

Endogenous Metabolite (4)

FGFR (2)

GABA Receptor (1)

Histamine Receptor (4)

Histone Demethylase (1)

Isotope-Labeled Compounds (7)

mAChR (5)

Monoamine Oxidase (2)

p38 MAPK (2)

Potassium Channel (5)

Reference Standards (5)

Serotonin Transporter (9)

Sodium Channel (4)

TGF-β Receptor (2)

Trace Amine-associated Receptor (TAAR) (1)

Transthyretin (TTR) (2)

Trk Receptor (4)

By Research Areas:

Cancer (8)

Cardiovascular Disease (3)

Endocrinology (5)

Inflammation/Immunology (7)

Metabolic Disease (4)

Neurological Disease (29)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1473

Serotonin hydrochloride 30+ Cited Publications 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-B0527A

Amitriptyline hydrochloride 5+ Cited Publications	Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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-N1957

Gamma-Mangostin 2 Publications Verification γ-Mangostin	5-HT Receptor COX Transthyretin (TTR)	Metabolic Disease Inflammation/Immunology Cancer
Gamma-Mangostin is a novel competitive **5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2)** inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 ^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-B0527

Amitriptyline 5+ Cited Publications	Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline 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 is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with K_i = 2.58 μM). Amitriptyline 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 can block sodium channels and hERG potassium channel (IC₅₀ = 4.78 μM) and it has cardiotoxicity .

HY-15414A

Vortioxetine hydrobromide 5+ Cited Publications Lu AA21004 hydrobromide	5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-B1018A

Phenelzine sulfate 5+ Cited Publications	Monoamine Oxidase GABA Receptor Histone Demethylase	Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer .

HY-A0019A

Paliperidone palmitate 1 Publications Verification 9-Hydroxyrisperidone palmitate	Dopamine Receptor 5-HT Receptor	Neurological Disease
Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and **5-hydroxytryptamine 2A (5-HT2A) receptors** that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-10351A

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

HY-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-15472

PRX-08066	5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase	Cardiovascular Disease Neurological Disease Cancer
PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .

HY-B0189B

Mosapride citrate dihydrate 5+ Cited Publications TAK-370 citrate dihydrate; AS-4370 citrate dihydrate	5-HT Receptor Potassium Channel Cytochrome P450	Metabolic Disease Cancer
Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with *5-hydroxytryptamine₄* receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC₅₀ values of 15.2 μM . Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo .

HY-B0527AR

Amitriptyline hydrochloride (Standard) 4 Publications Verification	Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. 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-B0527AS

Amitriptyline-d6 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis	Neurological Disease Inflammation/Immunology Endocrinology
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-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-15414AR

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

HY-15414S

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

HY-156807

LY 367265	Serotonin Transporter 5-HT Receptor	Neurological Disease
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .

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-B0884

Minaprine	Monoamine Oxidase Cholinesterase (ChE)	Neurological Disease
Minaprine is a brain-penetrant monoamine oxidase inhibitor. Minaprine also weakly inhibits acetylcholinesterase (AChE) activity. Minaprine reduces intraneuronal dopamine metabolism, lowers striatal homovanillic acid and dihydroxyphenylacetic acid levels, and raises striatal 3-methoxytyramine and 5-hydroxytryptamine levels. Minaprine exhibits convulsant, antidepressant properties .

HY-A0019AS

Paliperidone palmitate-d4 9-Hydroxyrisperidone palmitate-d₄	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

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-10351

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

HY-121562

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

HY-15414AS

Vortioxetine-d8 hydrobromide Lu AA21004-d8 hydrobromide	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine-d₈ (Lu AA 21004-d₈) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-136634

BTM-1042	mAChR	Others
BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guinea pig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.

HY-175285

5-HT2AR-IN-1	5-HT Receptor	Neurological Disease
5-HT_2AR-IN-1 (Compound Ie) is an orally active 5-hydroxytryptamine 2A receptor (5-HT_2AR) inhibitor with antidepressant efficacy. 5-HT_2AR-IN-1 reduces 5-HT_2AR expression and SERT protein levels. 5-HT_2AR-IN-1 is promising for research of central nervous system (CNS), such as depression and addiction-related disorders .

HY-N1957R

Gamma-Mangostin (Standard) γ-Mangostin (Standard)	Reference Standards 5-HT Receptor COX Transthyretin (TTR)	Metabolic Disease Inflammation/Immunology Cancer
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-118727

6-APDB hydrochloride	Trace Amine-associated Receptor (TAAR) 5-HT Receptor	Neurological Disease
6-APDB hydrochloride is a trace amine-associated receptor 1 agonist. It is also a regulator of 5-hydroxytryptamine receptor and a inhibitor of sodium-dependent noradrenaline transporter inhibitor.

HY-A0019AR

Paliperidone palmitate (Standard) 9-Hydroxyrisperidone palmitate (Standard)	Dopamine Receptor 5-HT Receptor Reference Standards	Neurological Disease
Paliperidone palmitate (Standard) is the analytical standard of Paliperidone palmitate. This product is intended for research and analytical applications. Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-W982195

Napamezole hydrochloride	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Napamezole hydrochloride is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with K_i values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole hydrochloride can be used for the research of depression .

HY-106605S

Flumezapine-d8 hydrochloride LY 120363-d8 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
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-19927A

DA-6886 monohydrochloride	5-HT Receptor	Neurological Disease Endocrinology
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC₅₀ value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .

HY-15472A

PRX-08066 maleate	5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase	Cardiovascular Disease Neurological Disease Cancer
PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .

HY-148032

5-Benzyloxytryptamine 5-BT	5-HT Receptor	Neurological Disease
5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT₁D/₁B) receptors with an IC₅₀ value of 40 nM for bovine caudate 5-HT₁D and reduced affinity for other receptors (5-HT₂ IC₅₀>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B1473

Serotonin hydrochloride 30+ Cited Publications 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-N1957

Gamma-Mangostin 2 Publications Verification γ-Mangostin	Xanthones Classification of Application Fields Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Metabolic Disease Plants Disease Research Fields	5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin is a novel competitive **5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2)** inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 ^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

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-N1957R

Gamma-Mangostin (Standard) γ-Mangostin (Standard)	Structural Classification Xanthones Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Plants	Reference Standards 5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

Cat. No.	Product Name	Chemical Structure

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-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.

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-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-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-A0019AS

Paliperidone palmitate-d4
Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

Paliperidone palmitate-d4

Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

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-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.

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