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GBR 12935
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GBR 12935图片
CAS NO:76778-22-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
GBR 12935是一种有效的选择性多巴胺再摄取抑制剂,在 COS-7 细胞中与多巴胺转运体的结合常数 Kd为 1.08 nM。GBR 12935 对不同品系小鼠的运动活性均有刺激作用,但对刻板印象无诱导作用。并且,GBR 12935 也可以防止 d-芬氟拉明诱导的小鼠头抽搐反应。
生物活性

GBR 12935 is a potent, and selectivedopaminereuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice[1][2][3][4].

体外研究
(In Vitro)

GBR 12909 (10-100 nM) also shows a high affinity for CYP2D6 with the Kdvalue of 42.2 nM, lower than the affinity for dopamine transporter. The binding effect can be reduced byQuinidine(HY-B1751) andQuinine(HY-D0143), which are the specific and potent inhibitors of CYPZD enzymatic activities[1].
GBR 12935 (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens[2].
GBR 12935 (100 μM; 60 min) increases extracellular levels of dopamine compared with levels for artificial cerebrospinal fluid (ACSF) by local perfusion for 60 min[2].
GBR 12935 (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens[2].
Co-perfusion of 100 μM GBR 12935 with either 100 μMSulpiride(HY-B1019) orRaclopride(HY-103414) produces a significant reduction in the GBR 12935 induced increase in the extracellular levels of dopamine to basal levels[2].

体内研究
(In Vivo)

GBR 12935 (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[3].

Animal Model:Adult male DBA/2J and C57BL/6J mice (22-30 g)[3]
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 in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.
分子量

414.58

Formula

C28H34N2O

CAS 号

76778-22-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.