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.
For research use only. We do not sell to patients.
- CAS No.: 76778-22-8
- Formula: C28H34N2O
- Molecular Weight:414.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) GBR 12935
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Biological Activity
Description
Cellular Effect
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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] |
In Vitro
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. .
In Vivo
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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Molecular Weight 414.58
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
Purity & Documentation
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. [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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GBR 12935 Related Classifications
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