产品
编 号:F398107
分子式:C17H22Cl3N5
分子量:402.75
产品类型
结构图
CAS No: 587870-77-7
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产品详情
生物活性:
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
体内研究:
ABT-724 (8.8 μg/kg; subcutaneous injection; daily; for 5 days; male adult Wistar rats) treatment dose-dependently facilitates penile erection when given s.c. to conscious rats.Animal Model:Male adult Wistar rats (~300 g)
Dosage:8.8 μg/kg
Administration:Subcutaneous injection; daily; for 5 days
Result:Dose-dependently facilitated penile erection.
体外研究:
ABT-724 exhibits a selective biochemical profile, as indicates by a lack of binding affinity for >70 neurotransmitter/uptake/ion channels including D2, D3, or D5 receptors up to a 10 μM concentration. A weak affinity to 5-HT1A receptors (Ki = 2780 nM) is observed. ABT-724 does not inhibit the PDE activity of PDE1, PDE5, or PDE6 at 10 μM concentrations.