| 产品描述： | GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice |
| 靶点： |
Dopamine Transporter;DopamineReceptor |
| 体内研究： |
GBR 12935 dihydrochloride (1-32 mg/kg; repeat injection; 7 d) elevates locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice, and (10 mg/kg; injection; 7 d) results few mice sensitized to cocaine-induced stereotypy with repeated injections Animal Model: Adult male DBA/2J and C57BL/6J mice (22-30 g) Dosage: 1.0, 3.2, 10, 32 mg/kg Administration: Repeat injection; for 7 days Result: Elevated locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice.No stereotypy was induced by an eighth day challenge of 10 mg/kg GBR 12935 dihydrochloride in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline. |
| 参考文献： |
1. Hiroi T, et al. Specific binding of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl propyl) piperazine (GBR-12935), an inhibitor of the dopamine transporter, to human CYP2D6. Biochem Pharmacol. 1997 Jun 15;53(12):1937-9. 2. Rahman S, et al. Negative interaction of dopamine D2 receptor antagonists and GBR 12909 and GBR 12935 dopamine uptake inhibitors in the nucleus accumbens. Eur J Pharmacol. 2001 Feb 23;414(1):37-44. 3. Tolliver BK, et al. Comparison of cocaine and GBR 12935: effects on locomotor activity and stereotypy in two inbred mouse strains. Pharmacol Biochem Behav. 1994 Jul;48(3):733-9. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.051 ml |
10.256 ml |
20.513 ml |
| 5 mM |
0.41 ml |
2.051 ml |
4.103 ml |
| 10 mM |
0.205 ml |
1.026 ml |
2.051 ml |
| 50 mM |
0.041 ml |
0.205 ml |
0.41 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