Cas No.: | 726174-00-1 |
Chemical Name: | 1H-Benzimidazole, 2-[[4-(3,4-dimethylphenyl)-1-piperazinyl]methyl]- |
Synonyms: | 1H-Benzimidazole, 2-[[4-(3,4-dimethylphenyl)-1-piperazinyl]methyl]-;A-381393 |
SMILES: | CC1C(C)=CC=C(N2CCN(CC3=NC4=CC=CC=C4N3)CC2)C=1 |
Formula: | C20H24N4 |
M.Wt: | 320.431 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1]. |
Target: | A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1]. |
In Vitro: | A-381393 exhibits weak affinity at 5-HT1A, Sigma 2, Adenoceptor α1A, Adenoceptor α2C, Histamine H1, with Kis of 1365, 8600, 2044, 1912 and 2962 nM, respectively[1]. |
References: | [1]. Nakane M, et al. 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist. Neuropharmacology. 2005 Jul;49(1):112-21. |