GBR 12935
Based on 1 publication(s) in Google Scholar
GBR 12935 is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice.
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- CAS No.: 76778-22-8
- Formule: C28H34N2O
- Masse moléculaire:414.58
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) GBR 12935
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.018 μM
Compound: GBR-12935
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Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter
Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter
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[PMID: 10649976] |
| HEK293 | IC50 |
0.165 μM
Compound: GBR-12935
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Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells
Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells
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[PMID: 10649976] |
| HEK293 | IC50 |
3.71 μM
Compound: GBR-12935
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Inhibition of [3H]5-HT reuptake in HEK293 cells expressing human serotonin transporter
Inhibition of [3H]5-HT reuptake in HEK293 cells expressing human serotonin transporter
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[PMID: 10649976] |
GBR 12909 (10-100 nM) also shows a high affinity for CYP2D6 with the Kd value of 42.2 nM, lower than the affinity for dopamine transporter. The binding effect can be reduced by Quinidine (HY-B1751) and Quinine (HY-D0143), which are the specific and potent inhibitors of CYPZD enzymatic activities[1].
GBR 12935 (10 nM; 2 min) increases the extracellular levels of dopamine to approximately 400% of basal during the application in the nucleus accumbens[2].
GBR 12935 (100 μM; 60 min) increases extracellular levels of dopamine compared with levels for artificial cerebrospinal fluid (ACSF) by local perfusion for 60 min[2].
GBR 12935 (1-9 nM) dose-dependently inhibits active uptake of [3H]dopamine in homogenates of the nucleus accumbens[2].
Co-perfusion of 100 μM GBR 12935 with either 100 μM Sulpiride (HY-B1019) or Raclopride (HY-103414) produces a significant reduction in the GBR 12935 induced increase in the extracellular levels of dopamine to basal levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male DBA/2J and C57BL/6J mice (22-30 g)[3]
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Dosage:1.0, 3.2, 10, 32 mg/kg
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Administration:Repeat injection; for 7 days
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Result:Elevated locomotion activity to a greater extent in C57BL/6J mice than DBA/2J mice.
No stereotypy was induced by an eighth day challenge of 10 mg/kg GBR 12935 in mice pretreated with seven dally injections of either 32 mg/kg cocaine or saline.
Chemical Information
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CAS No. 76778-22-8
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Masse moléculaire 414.58
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Formule C28H34N2O
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SMILES
N1(CCOC(C2=CC=CC=C2)C3=CC=CC=C3)CCN(CCCC4=CC=CC=C4)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[4]. Darmani NA. Cocaine and selective monoamine uptake blockers (sertraline, nisoxetine, and GBR 12935) prevent the d-fenfluramine-induced head-twitch response in mice. Pharmacol Biochem Behav. 1998 May;60(1):83-90. [Content Brief]
Calculators
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GBR 12935 Related Classifications
HY-12242A Related Classifications
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