GBR 12935

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

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].

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

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	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.

Description

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.

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℃

HS Code	2933599090

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%

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

DC Chemicals Limited
China
Product Name: GBR 12935
Price: $100.0/100mg $200.0/250mg $400.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 1-(2-(BENZHYDRYLOXY)ETHYL)-4-(3-PHENYLPROPYL)PIPERAZINE MALEATE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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GBR 12935

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