GBR 12935

Cas No.:	76778-22-8
Chemical Name:	Piperazine, 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-
Synonyms:	GBR12935;GBR-12935
SMILES:	C(O)(=O)/C=C/C(O)=O.C(OCCN1CCN(CCCC2C=CC=CC=2)CC1)(C1C=CC=CC=1)C1C=CC=CC=1
Formula:	C28H34N2O
M.Wt:	414.5824

Description:	GBR 12935 is a potent, and selective dopamine reuptake inhibitor.
In Vivo:	GBR 12935 elevated locomotion to a greater extent in C57BL/6J mice at the maximally active dose of 10 mg/kg. Locomotor stimulation by GBR 12935 remained consistent in both strains with repeated injections. DBA/2J mice became sensitized to cocaine-induced stereotypy with repeated injections. Cocaine induced no stereotypy in C57BL/6J mice on any test day. No stereotypies were induced by GBR 12935 in either strain on any test day [3].
In Vitro:	The calculated Kd of [3H]GBR-12935 binding to CYP2D6 was 42.2 nM, indicating that GBR-12935 has a high affinity for CYP2D6. The binding of [3H]GBR-12935 to CYP2D6 was decreased partially by substrates or inhibitors of CYP2D isoforms (quinine, quinidine, propranolol, bufuralol, imipramine, and desipramine) [1]. Co-perfusion of 100 microM GBR 12909 or GBR 12935 with either 100 microM 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. In vitro, GBR 12909 (1-9 nM) dose-dependently inhibited active uptake of [3H]dopamine in homogenates of the nucleus accumbens [2].