GBR 12935

Modify Date: 2024-01-02 08:55:18

GBR 12935 Structure
GBR 12935 structure
Common Name GBR 12935
CAS Number 76778-22-8 Molecular Weight 414.58
Density 1.067g/cm3 Boiling Point 540.6ºC at 760 mmHg
Molecular Formula C28H34N2O Melting Point N/A
MSDS N/A Flash Point 143.9ºC

 Use of GBR 12935


GBR 12935 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].

 Names

Name 1-[2-(benzhydryloxy)ethyl]-4-(3-phenylpropyl)piperazine
Synonym More Synonyms

 GBR 12935 Biological Activity

Description GBR 12935 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
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.

 Chemical & Physical Properties

Density 1.067g/cm3
Boiling Point 540.6ºC at 760 mmHg
Molecular Formula C28H34N2O
Molecular Weight 414.58
Flash Point 143.9ºC
PSA 90.31000
LogP 4.63060
Index of Refraction 1.576
Storage condition 2-8℃

 Safety Information

HS Code 2933599090

 Customs

HS Code 2933599090
Summary 2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2Z)-but-2-enedioate (1:1)
Piperazine, 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-, (2Z)-2-butenedioate (1:1)
1-[2-(Diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (2Z)-2-butenedioate (1:1)
1-(2-benzhydryloxy-ethyl)-4-(3-phenyl-propyl)-piperazine
Piperazine,1-(2-(diphenylmethoxy)ethyl)-4-(3-phenylpropyl)
N-[3-tert-Butyl-1-(4-Methylphenyl)-1H-pyrazol-5-yl]-N-[4-[2-(4-Morpholinyl)ethoxy]naphthalen-1-yl]urea
1-Hydrocinnamyl-4-[2-(diphenylmethoxy)ethyl]piperazine
1-(2-(diphenylmethoxy)-ethyl)-4-(3-phenylpropyl)piperazine
1-(2-(Benzhydryloxy)ethyl)-4-(3-phenylpropyl)piperazine maleate
GBR 12935
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