5-HT Receptor Inhibitor

5-HT Receptor Inhibitors (96):

Cat. No.	Product Name	Effect	Purity

HY-N0737A

Harmine	Inhibitor	99.88%
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (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-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 (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-15414A

Vortioxetine hydrobromide	Inhibitor	99.91%
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-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-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-101456

PCPA methyl ester hydrochloride	Inhibitor	99.89%
PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability.

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-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-14557A

Pimavanserin hemitartrate	Inhibitor	99.91%
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-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-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-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-W011235

Norfluoxetine hydrochloride	Inhibitor	99.58%
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-U00096

Ansofaxine hydrochloride	Inhibitor	99.72%
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-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-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-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-125784

Viloxazine hydrochloride	Inhibitor	98.94%
Viloxazine hydrochloride is the hydrochloride salt form of Viloxazine (HY-W380450). Viloxazine (Viloxazin) hydrochloride is a norepinephrine reuptake inhibitor and a potent 5-HT_2C agonist agent and 5-HT_2B antagonist, EC₅₀ for 5-HT_2C b> is 32 μM, and the IC₅₀ for 5-HT_2B is 27 μM. Viloxazine hydrochloride's mechanism of action primarily involves serotonergic and noradrenergic pathways. Viloxazine hydrochloride is used in antidepressant research.

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.

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