Biological Activity
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].
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
In Vivo
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]. Animal Model: Male Sprague-Dawley rats[1] Dosage: 3.7, 11, 33, or 100 µmol/kg (synthesized in-house as HCl salt, was dissolved in physiologic saline (0.9% w/v NaCl) Administration: s.c. was administered subcutaneously 4 min before the start of recording Result: Dose-dependently inhibited the behavioral activation following pretreatment with D-amphetamine or MK-801.
References & source
[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.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.