5-HT Receptor Inhibitor

Azatadine is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine induces sedation and exhibits topical anesthetic properties. Azatadine can be used for the research of allergic rhinitis.

Proxibarbal is a barbiturate derivative. Proxibarbal has anti-anxiety properties and is also used for the study of migraine headaches.

Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.

5-APDI hydrochloride is an indane with an amphetamine-like aminopropane group. 5-APDI hydrochloride inhibits the uptake of serotonin, dopamine, and norepinephrine by crude synaptosomes (IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively).

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).

BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with K_i of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABA_A receptor with K_i of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (K_i is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate.

Fluvoxamino acid is the major metabolite of Fluvoxamine (HY-B0103) produced in the human body, and acts as a 5-HT reuptake transporter inhibitor. Fluvoxamino acid exhibits weaker inhibitory activity against 5-HT reuptake than its parent compound Fluvoxamine, and can synergistically regulate 5-HT transmission with the parent compound. Fluvoxamino acid can be used in the research of major depressive disorder.

Dotarizine is a novel Piperazine (HY-B0912) derivative and antimigraine agent. Dotarizine exhibits Ca²⁺ channel blocking properties. Dotarizine decreases the release of lactate dehydrogenase. Dotarizine shows 5-HT receptor blocking effect.

Oxatomide (Standard) (KW-4354 (Standard)) is the analytical standard of Oxatomide (HY-123205). This product is intended for research and analytical applications. Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.

Melitracen-d₆ (hydrochloride) is the deuterium labeled Melitracen hydrochloride. 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.

Tiprenolol hydrochloride is a β-adrenoceptor blocker. Tiprenolol hydrochloride abolished ventricular arrhythmias induced by intravenous epinephrine in dogs receiving halothane inhalation.

5-HT3-In-1 is extracted from patent EP0748807A1, compound example 8. It shows 5-HT3 inhibition activity.