5-HT Receptor Inhibitor

Paroxetine (BRL29060) mesylate is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine mesylate inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine mesylate is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine mesylate is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

5-HT2A inverse agonist-1 is a 5-HT_2A receptor inverse agonist with a IC₅₀ of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease.

PUC-55 is a 5-HT₆R antagonist with a K_i of 37.5 nM that induces neuronal autophagy by inhibiting the mTOR pathway. It holds potential for research in the field of neurological disorders.

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.

Pridefine (AHR-1118) is an antidepressant agent.

Citalopram hydrochloride is an orally active 5-HT Receptor inhibitor. Citalopram hydrochloride can be used in depression research.

(R)-Viloxazine hydrochloride is the less active R-isomer of Viloxazine hydrochloride (HY-125784). (R)-Viloxazine hydrochloride can be used in the research of depression.

Cyproheptadine-d₃ is the d₃-labeled Cyproheptadine (HY-B1622). Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.

(R)-Venlafaxine is the R-enantiomer of venlafaxine (HY-B0196), an orally active and potent dual inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake. (R)-Venlafaxine can be utilized in antidepressant research.

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.

Butriptyline (Butriptylene) is an orally active tricyclic antidepressant that slightly enhances central 5-HT effects. Butriptyline does not inhibit brain norepinephrine uptake. Butriptyline can be used for depression research.

Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline.

(S)-AS1069562 is the S-enantiomer of AS1069562 (HY-138257A). AS1069562 is an orally active 5-HT and NE reuptake inhibitor, with IC₅₀ values of 0.35 μM and 3.3 μM, respectively. AS1069562 possesses curative-like analgesic effect. AS1069562 might improve nerve function impairment via the amelioration of neurotrophic support.

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).

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

4-Chloromethamphetamine hydrochloride is a new psychoactive substance belonging to the amphetamine class.

Cianopramine hydrochloride (Cyanimipramine hydrochloride; Ro 11-2465 hydrochloride) is the hydrochloride form of Cianopramine (HY-101753). Cianopramine hydrochloride is an antidepressant, which selectively inhibits the serotonin uptake into synaptosomes.

PIM-35 is a derivative of Indole (HY-W001132). PIM-35 significantly inhibits serotonin (5HT) and dopamine (DA) uptake with a weak inhibitory effect on noradrenaline (NA) uptake.PIM-35 has antidepressant activity and can be used for depression research.

Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow.