A-381393

Modify Date: 2024-01-07 22:32:06

A-381393 Structure
A-381393 structure
Common Name A-381393
CAS Number 726174-00-1 Molecular Weight 320.43
Density N/A Boiling Point N/A
Molecular Formula C20H24N4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of A-381393


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].

 Names

Name A-381393

 A-381393 Biological Activity

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].
Related Catalog
Target

Ki: 1.5 nM (D4.4 receptor), 1.9 nM (D4.2 receptor), 1.6 nM (D4.7 receptor)[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.

 Chemical & Physical Properties

Molecular Formula C20H24N4
Molecular Weight 320.43
Storage condition 2-8℃
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