Serotonin Transporter Antagonist

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.

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.

Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT_2A (K_i=2.89, 0.54 and 2.5 nM for rat 5-HT_2A, rabbit 5-HT_2A and human 5-HT_2A, respectively).

SERT/NET-IN-1 is a blood-brain barrier-permeable SERT and NET inhibitor, with an IC₅₀ of 11.2 nM against human SERT and an IC₅₀ of 32.0 nM against human NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET-IN-1 can be used in studies related to premature ejaculation.

NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC₅₀ = 0.3 μM) and monoamine transporter activities (SERT IC₅₀ = 1.1 μM、DAT IC₅₀ = 0.7 μM、NET IC₅₀ = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC₅₀ > 100 μM); cardiotoxicity (IC₅₀ = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression.

Trazodone (AF-1161 free base) (Standard) is the analytical standard of Trazodone. This product is intended for research and analytical applications. Trazodone 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.

Glemanserin (Standard) is the analytical standard of Glemanserin. This product is intended for research and analytical applications. Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively).