GBR 12935 (fumarate)

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

Product Specifications

CAS Number

[1349767-56-1]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Dopamine Transporter

Type

Reference compound

Related Pathways

Neuronal Signaling

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gbr-12935-fumarate.html

Smiles

O=C(O)/C=C\C(O)=O.N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(CCCC4=CC=CC=C4)CC1

Molecular Formula

C32H38N2O5

Molecular Weight

530.65

Precautions

P261-P280-P302+P352

References & Citations

[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.|[4]Darmani NA. Cocaine and selective monoamine uptake blockers (sertraline, nisoxetine, and GBR 12935) prevent the d-fenfluramine-induced head-twitch response in mice. Pharmacol Biochem Behav. 1998 May;60 (1) :83-90.