产品
编 号:F175456
分子式:C19H26ClN3
分子量:331.88
产品类型
结构图
CAS No: 149654-41-1
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产品详情
生物活性:
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM).
体内研究:
U92016A (U-92016A) potently decreases rectal temperature in mice. U92016A also elicits the 5-HT-mediated syndrome in rats and results in a dose-related decrease in 5-hydroxytryptophan accumulation. U92016A also decreases arterial blood pressure in spontaneously hypertensive rats and inhibits sympathetic nerve activity in cats. U92016A displays excellent potency and a long duration of action. U92016A also inhibits the firing of dorsal raphe 5-HT neurons and is active in two social interaction assays. The p.o. bioavailability of U92016A is 45%.
体外研究:
U92016A (U-92016A) is selective for the 5-HT1A receptor over other biogenic amine receptors. U92016A decreases the Forskolin-induced increase in cyclic AMP synthesis and has an intrinsic activity of 0.82 relative to 5-HT in Chinese hamster ovary cells expressing the human 5HT1A receptor.