Cas No.: | 2562346-14-7 |
Chemical Name: | Mesdopetam hemitartrate |
SMILES: | OC([C@H](O)[C@@H](O)C(O)=O)=O.CCCNCCOC1=CC(S(C)(=O)=O)=CC(F)=C1.[1/2] |
Formula: | C12H18FNO3S.1/2C4H6O6 |
M.Wt: | 700.77 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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 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: | [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. |