S88231 |
AZD-6280 |
源叶(MedMol) | 98% |
- 产品描述: AZD6280 is a novel, subtype-selective GABAAα2/3 receptor positive modulators, used for treatment of generalized anxiety disorder.
- 靶点: GABA Receptor;GABAReceptor
- 体内研究:
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
- 动物实验: 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
- 参考文献:
1. Jucaite A , Cselényi, Zsolt, Lappalainen J , et al. GABAAreceptor occupancy by subtype selective GABAAα2,3modulators: PET studies in humans[J]. Psychopharmacology, 2017, 234(4):707-716. 2. Te Beek E T , Chen X , Jacobs G E , et al. The effects of the nonselective benzodiazepine lorazepam and the α2 /α3 subunit-selective GABAA receptor modulators AZD7325 and AZD6280 on plasma prolactin levels.[J]. Clin Pharmacol Drug Dev, 2015, 4(2):149-154.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.729 ml 13.646 ml 27.292 ml 5 mM 0.546 ml 2.729 ml 5.458 ml 10 mM 0.273 ml 1.365 ml 2.729 ml 50 mM 0.055 ml 0.273 ml 0.546 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)