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GBR 12935 2HCl

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Chemical Structure| 67469-81-2 同义名 : GBR 12935 (hydrochloride);GBR 12935 dihydrochloride
CAS号 : 67469-81-2
货号 : A751627
分子式 : C28H36Cl2N2O
纯度 : 98%
分子量 : 487.504
MDL号 : MFCD00083175
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(51.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 7 mg/mL(14.36 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor. The calculated Kd of [3H]GBR-12935 binding to CYP2D6 was 42.2 nM[3]. Co-perfusion of 100 mM GBR 12909 or GBR 12935 with either 100 mM sulpiride or raclopride produced a significant reduction in the GBR 12909 or GBR 12935 induced increase in the extracellular levels of dopamine to basal levels[4]. GBR 12935 elevated locomotion to a greater extent in C57BL/6J mice at the maximally active dose of 10 mg/kg[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.26mL

2.05mL

1.03mL

20.51mL

4.10mL

2.05mL
参考文献

[1]Rahman S, Engleman E, 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.

[2]Hiroi T, Imaoka S, 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.

[3]Hiroi T, Imaoka S, Chow T, Yabusaki Y, Funae Y. 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

[4]Rahman S, Engleman E, Simon J, McBride WJ. 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

[5]Tolliver BK, Carney JM. 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