GBR 12935 (dihydrochloride)

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[1][2][3][4].

Product Specifications

CAS Number

[67469-81-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Dopamine Transporter

Type

Reference compound

Related Pathways

Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/GBR-12935-dihydrochloride.html

Purity

99.80

Solubility

DMSO : 25 mg/mL (ultrasonic) |H2O : 7.14 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(CCCC4=CC=CC=C4)CC1.Cl.Cl

Molecular Formula

C28H36Cl2N2O

Molecular Weight

487.50

Precautions

H302, H315, H319, H335

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.