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GBR 12935 dihydrochloride

Names

[ CAS No. ]:
67469-81-2

[ Name ]:
GBR 12935 dihydrochloride

[Synonym ]:
1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride
Piperazine, 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-, hydrochloride (1:2)
1-(2-DIPHENYLMETHOXYETHYL)-4-(3-PHENYLPROPYL)PIPERAZINE DIHYDROCHLORIDE
GBR 12935 dihydrochloride
GBR 12935 (dihydrochloride)

Biological Activity

[Description]:

GBR 12935 2Hcl is a potent, and selective dopamine reuptake inhibitor.IC50 value: Target: dopamine reuptake inhibitorin 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].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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Dopamine Transporter
Research Areas >> Neurological Disease

[References]

[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.


[Related Small Molecules]

Vanoxerine dihydrochloride | Fipexide | Dasotraline (hydrochloride) | Diclofensine (hydrochloride) | GBR 12935 | Levophacetoperane (hydrochloride) | SPD-473 citrate | Centanafadine Hydrochloride

Chemical & Physical Properties

[ Boiling Point ]:
564ºC at 760 mmHg

[ Molecular Formula ]:
C28H36Cl2N2O

[ Molecular Weight ]:
487.504

[ Flash Point ]:
294.9ºC

[ Exact Mass ]:
486.220459

[ PSA ]:
15.71000

[ LogP ]:
6.52280

[ Appearance of Characters ]:
white solid

[ Storage condition ]:
-20℃

MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Articles

Plasma membrane monoamine transporters: structure, regulation and function.

Nat. Rev. Neurosci. 4 , 13-25, (2003)

Studies of the biogenic amine transporters. III. Demonstration of two binding sites for [3H]GBR12935 and [3H]BTCP in rat caudate membranes.

J. Pharmacol. Exp. Ther. 268 , 1462-1475, (1994)

The present study addressed the hypothesis that there exist multiple sites/states associated with the dopamine (DA) transporter ligands. The authors used [3H](1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylp...

[3H]GBR-12935 binding to cytochrome P450 in the human brain.

J. Neurochem. 62 , 342-348, (1994)

The presence of multiple [3H]GBR-12935 binding sites in the human brain has been revealed in several recent studies. One site represents the dopamine uptake site. In rat brain it was demonstrated that...


More Articles


Related Compounds