Гидрохлорид Нефазодон

Описание

Nefazodone, a second generation trazodone type antidepressant, was launched in Canada. Nefazodone acts as both a potent 5-HT₂ receptor antagonist and as a serotonin (5-HT) reuptake inhibitor. This combination effect appears to enhance 5-HT_IA-mediated neurotransmission. Distinct from the first generation agents such as tricyclic antidepressants, nefazodone has very selective serotonergic effects with negligible affinity for cholinergic and histamine receptors, and low affinity for a₁ -adrenergic receptors. Therefore, it has a superior toxicity profile that does not produce agitation, insomnia, and lacks cardiac side effects.

Химические свойства

White Solid

Использование

A selective serotonin 5-HT2 receptor antagonist. A novel antidepressant that shows no cardiac toxicity or anticholinergic activity common with tricyclic antidepressants.

Общее описание

Nefazodone, formerly sold under the brand names Serzone, Dutonin, and Nefadar, is an antidepressant that has been discontinued due to the incidence of severe liver damage. This certified Snap-N-Spike^; solution is suitable for use as a starting material in calibrators and controls for numerous GC/MS or LC/MS applications in forensic analysis, clinical toxicology and urine drug testing.

Биологическая активность

Serotonin 5-HT 2A receptor antagonist (K i = 5.8 nM) and inhibitor of serotonin and noradrenalin uptake (IC 50 values are 290 and 300 nM respectively). Displays no activity at 5-HT 1B and 5-HT 1D receptors. Active in models predictive of antidepressant potential.