产品
编 号:F288751
分子式:C11H14Cl2N2O
分子量:261.15
产品类型
结构图
CAS No: 2414674-71-6
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产品详情
生物活性:
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
体内研究:
SUVN-911 is devoid of cardiovascular and gastrointestinal side effects.SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects.SUVN-911 shows metabolic stability in rats.SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats.Animal Model:Male Wistar rats (180-230 g)
Dosage:1 mg/kg, 3 mg/kg, 10.0 mg/kg
Administration:Oral administration, daily, for 3 days
Result:Showed antidepressant like activity with no signs of tachyphylaxis.
Animal Model:Male Wistar rats (225 ± 25 g)
Dosage:3 mg/kg (Pharmacokinetic Analysis)
Administration:Oral administration
Result:AUC=3507 ng*h/mL, T1/2=3.34 hours.
体外研究:
SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR.SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins.