AHN 1-055 hydrochloride

AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT) and may serve as leads for the development of agentia to treat cocaine abuse[1].

Signaling Pathways >> Neuronal Signaling >> Dopamine Transporter

Research Areas >> Neurological Disease

IC50: 71 nM (dopamine uptake)[1]

AHN 1-055 (5 mg/kg; i.v.) inhibits the uptaking of brain dopamine with an IC50 of 311.8 ng/ml in vivo[1]. AHN 1-055 (10 mg/kg; i.v.) exhibits Cmax of 1.48 mg/L and terminal elimination half-lives of 7.69 h due to 1.8L/h/kg plasma clearance combined with 18.7 L/kg volumes of distribution[1]. Animal Model: Adult male Sprague Dawley rats (250-275 g)[1] Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: I.v. administration Result: Cmax (1.48 mg/L); T1/2 (7.69 h).

[1]. Sangeeta R, et, al. Investigation of the potential pharmacokinetic and pharmaco-dynamic drug interaction between AHN 1-055, a potent benztropine analog used for cocaine abuse, and cocaine after dosing in rats using intracerebral microdialysis. Biopharm Drug Dispos. 2006 Jul; 27(5): 229-40.