| Identification | Back Directory | [Name]
Mesdopetam L-tartrate salt | [CAS]
2562346-14-7 | [Synonyms]
IRL790 hemitartrate
Mesdopetam hemitartrate
Mesdopetam L-tartrate salt
3-?dihydroxybutanedioat?e (2:1)
N-?[2-?[3-?fluoro-?5-?(methylsulfonyl)?phenoxy]?ethyl]?-
1-?Propanamine, N-?[2-?[3-?fluoro-?5-?(methylsulfonyl)?phenoxy]?ethyl]?-?, (2R,?3R)?-?2,?3-?dihydroxybutanedioat?e (2:1) | [Molecular Formula]
C16H24FNO9S | [MOL File]
2562346-14-7.mol | [Molecular Weight]
425.42 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 20.83 mg/mL (29.72 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
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]. | [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]. | 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.
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| [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. |
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