GBR 12935 dihydrochloride
Modify Date: 2024-01-03 14:49:17
GBR 12935 dihydrochloride structure
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Common Name | GBR 12935 dihydrochloride | ||
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| CAS Number | 67469-81-2 | Molecular Weight | 487.504 | |
| Density | N/A | Boiling Point | 564ºC at 760 mmHg | |
| Molecular Formula | C28H36Cl2N2O | Melting Point | N/A | |
| MSDS | USA | Flash Point | 294.9ºC | |
Use of GBR 12935 dihydrochlorideGBR 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]. |
| Name | 1-(2-benzhydryloxyethyl)-4-(3-phenylpropyl)piperazine,dihydrochloride |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| References |
| Boiling Point | 564ºC at 760 mmHg |
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| 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℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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GBR 12935 dihyd... CAS#:67469-81-2 |
| Literature: Van Der Zee; Koger; Gootjes; Hespe European Journal of Medicinal Chemistry, 1980 , vol. 15, # 4 p. 363 - 370 |
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Plasma membrane monoamine transporters: structure, regulation and function.
Nat. Rev. Neurosci. 4 , 13-25, (2003)
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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... |
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[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... |
| 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) |