5-HT Receptor Inhibitor

5-HT Receptor Inhibitors (69):

Cat. No.	Product Name	Effect	Purity

HY-11018

Risperidone	Inhibitor	99.92%
Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-15414

Vortioxetine	Inhibitor	99.81%
Vortioxetine is a inhibitor of 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT, with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

HY-B0527A

Amitriptyline hydrochloride	Inhibitor	98.91%
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-15414A

Vortioxetine hydrobromide	Inhibitor	99.91%
Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

HY-14557

Pimavanserin	Inhibitor	99.86%
Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-10349A

WAY-100635 maleate	Inhibitor	99.89%
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 maleate has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D₄ receptor agonist.

HY-14557A

Pimavanserin hemitartrate	Inhibitor	99.75%
Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC₅₀ and pK_i of 8.73 and 9.3, respectively.

HY-112390A

Syk Inhibitor II	Inhibitor	98.05%
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.

HY-W019599

4-Chloro-L-phenylalanine	Inhibitor	≥98.0%
4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2).

HY-N0737

Harmine hydrochloride	Inhibitor	99.93%
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-119209

Nefazodone	Inhibitor	98.01%
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT_2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.

HY-123205

Oxatomide	Inhibitor	99.56%
Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC₅₀ of 0.95 μM). Oxatomide inhibits ATP-induced Ca²⁺ influx with an IC₅₀ value of 0.43 μM and also inhibits serotonin.

HY-U00096

Ansofaxine hydrochloride	Inhibitor	99.87%
Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC₅₀ values of 723, 491 and 763 nM, respectively.

HY-N0749A

Jatrorrhizine hydroxide	Inhibitor	98.07%
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.

HY-N0740

Jatrorrhizine chloride	Inhibitor	99.88%
Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC₅₀=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.

HY-B0352S

Mirtazapine-d₃	Inhibitor	98.55%
Mirtazapine-d₃ is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].

HY-108256

Melitracen hydrochloride	Inhibitor	99.90%
Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.

HY-W011235

Norfluoxetine hydrochloride	Inhibitor	99.27%
Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity.

HY-20696

Tetrahydro-β-carboline	Inhibitor
Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an K_i value of 6.1 µM.

HY-103094

LY266097 hydrochloride	Inhibitor	99.60%
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pK_is of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.

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