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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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