Mesdopetam (IRL790) hemitartrate 是一种多巴胺 D3 受体拮抗剂 (Ki=90 nM; IC50=9.8 μM)，具有稳定精神运动的特性。Mesdopetam hemitartrate 用于研究帕金森病的运动和精神并发症。
Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease[1][2].
Mesdopetam (IRL790) (3.7, 11, 33, or 100 µmol/kg; s.c.) hemitartrate dose-dependently inhibits the behavioral activation following pretreatment with D-amphetamine or MK-80[1].Mesdopetam (10 mg/kg; intraperitoneally; fourteen-week-old male C57BL/J mice) hemitartrate promotes a sedative effect similar to haloperidol with significantly reduced total distance traveled and reduced average speed[2].
[1]. Waters S, et al. Preclinical Pharmacology of [2-(3-Fluoro-5-Methanesulfonyl-phenoxy)Ethyl](Propyl)amine (IRL790), a Novel Dopamine Transmission Modulator for the Treatment of Motor and Psychiatric Complications in Parkinson Disease. J Pharmacol Exp Ther. 2020;374(1):113-125. [2]. Becanovic K, et al. Effects of a Novel Psychomotor Stabilizer, IRL790, on Biochemical Measures of Synaptic Markers and Neurotransmission. J Pharmacol Exp Ther. 2020;374(1):126-133.
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