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SB 277011A
- SB277011 dihydrochloride
Axon 1920
- Parent CAS: 215803-78-4
Purity:
99%
- Soluble in water and DMSO
- MF: C28H30N4O.2HCl
- MW: 511.49
Description
SB 277011A is a potent, selective and brain-penetrant dopamine D3 receptor antagonist with high affinity for the human D3 receptor.
D3 receptors are enriched in limbic circuits involved in reward, motivation and addiction-related behaviors. SB 277011A is used to study D3-selective dopamine pharmacology with substantial selectivity over D2 receptors and a broad receptor panel.
Key Features
- Selective dopamine D3 receptor antagonist
- Reported human D3 pKi: 7.95
- Approximately 100-fold selective over human D2 receptors
- Brain-penetrant tool for reward-circuit pharmacology
Applications
- Dopamine D3 receptor assays
- Addiction and reward-circuit research
- D3 versus D2 receptor selectivity studies
- CNS behavioral pharmacology models
More Information
| Parent CAS No. | 215803-78-4 |
|---|---|
| Chemical Name | N-((trans)-4-(2-(6-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)quinoline-4-carboxamide dihydrochloride |
| MFCD | MFCD16627999 |
| Short Description | D3 antagonist |
References
- G Stemp et al. Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist (...). J. Med. Chem. 2000, 43(9), 1878-1885.
- C Reavill et al. Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A. J. Pharmacol. Exp. Ther. 2000, 294(3), 1154-1165.
- E Southam et al. Effect of the selective dopamine D3 receptor antagonist SB-277011-A on regional c-Fos-like expression in rat forebrain. Brain Res. 2007, 1149, 50-57.
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