| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京