Mesdopetam

Mesdopetam (IRL790) is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease[1][2].

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

D3 Receptor

Mesdopetam (IRL790) (3.7, 11, 33, or 100 µmol/kg) 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) 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.

[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.