AZD-6280 是一种新型的亚型选择性 GABAAα2/3 受体阳性调节剂，用于治疗广泛性焦虑症。

AZD6280 is a novel, subtype-selective GABAAα2/3 receptor positive modulators, used for treatment of generalized anxiety disorder.

The [11C]flumazenil binding was reduced in a dose-dependent, saturable manner by AZD6280. Maximum receptor occupancy could be reached for AZD6280 without causing sedation or cognitive impairment. The K i,plasma estimates for AZD6280 was 440 nmol/l[1].

Two PET studies, using high-resolution research tomography (HRRT) and the radioligand [11C]flumazenil, were performed in 12 subjects at baseline and after administration of single oral doses of AZD7325 (0.2 to 30 mg) and AZD6280 (5 to 40 mg). PET images were analyzed using a simplified reference tissue model, and regional binding potentials (BPND) were obtained. The relationship between plasma concentration of AZD7325 or AZD6280 and GABAA receptor occupancy was described by hyperbolic function, and K i,plasma (plasma concentration required for 50% receptor occupancy) was estimated. Assessments of safety and tolerability included recording of adverse events, vital signs, electrocardiogram, and laboratory tests[1].

942436-93-3

C20H22N4O3

366.421

AZD-6280

DMSO:10mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years