5-HT Receptor Antagonist

PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC₅₀ of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT₃ receptor with an IC₅₀ of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems.

Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.

EEDQ is a carboxylate activator and irreversible antagonist of 5HT2c receptors. EEDQ reduces [³H]β-CIT binding to the dopamine transporter (DAT) in rat caudate-putamen (CPu) homogenates (IC₅₀ = 78.3 μM). EEDQ inhibits contralateral rotation behavior.

Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca²⁺ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca²⁺ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.

Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.

Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class.

TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.

SB-203186 hydrochloride is a potent, selective and competitive 5-HT₄ antagonist. SB-203186 hydrochloride antagonizes the 5-HT₄ receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pK_B values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.

Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.

Pirenperone (R 47465) is a 5-HT₂ serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity.

Ondansetron-d₅ is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT₃ receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.

Levomepromazine maleate (Methotrimeprazine maleate) is an orally active antipsychotic compound and Ca²⁺ release inducer. Levomepromazine maleate inhibits SERCA pump and induces an increase in cytoplasmic Ca²⁺ levels. Levomepromazine maleate has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine maleate can induce adaptive ER stress and autophagy. In addition, Levomepromazine maleate has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine maleate can be used in the study psychiatric disorders and relieving nausea and vomiting.

Marmin is a histamine receptor inhibitor and tracheal smooth muscle relaxant. Marmin antagonizes histamine- and methacholine-induced contraction of tracheal smooth muscle. Marmin inhibits histamine release from mast cells, and also blocks extracellular calcium influx via voltage-dependent calcium channels as well as calcium release from intracellular calcium stores, thereby effectively inhibiting calcium-mediated smooth muscle contraction. Marmin slightly enhances the relaxant effect of isoprenaline, and induces epithelial-dependent tracheal smooth muscle relaxation independent of nitric oxide, cGMP or β₂-adrenergic pathways through the release of prostaglandin E₂.

TDHL (Tergurid) is a dopamine receptor agonist with a K_d of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.

Trazodone (hydrochloride) (Standard) is the analytical standard of Trazodone (hydrochloride). This product is intended for research and analytical applications. Trazodone (hydrochloride) (AF-1161) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.

Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties.

Cyclobenzaprine (MK130) hydrochloride (Standard) is the analytical standard of Cyclobenzaprine (MK130) hydrochloride. This product is intended for research and analytical applications. Cyclobenzaprine hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases

Lerisetron is a potent 5-HT₃ antagonists and possess high-affinity binding for the 5-HT₃ receptors with pK_i value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats.

Ampreloxetine (TD-9855) TFA is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine TFA has the potential for the research of neurogenic orthostatic hypotension.