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

[11C]flumazenil的结合通过AZD6280以剂量依赖性和饱和性方式降低。AZD6280能达到最大受体占有率而不引起镇静或认知损害。AZD6280的K i,plasma估计为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].