Armesocarb
Chemical compound
From Wikipedia, the free encyclopedia
Armesocarb (developmental code name MLR-1019), also known as (R)-mesocarb or L-mesocarb, is a selective atypical dopamine reuptake inhibitor (DRI). It is currently under development for the treatment of Parkinson's disease and sleep disorders.[1][2]
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| Other names | (R)-Mesocarb; L-Mesocarb; MLR-1019; MLR1019 |
| Drug class | Atypical dopamine reuptake inhibitor |
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| Formula | C18H18N4O2 |
| Molar mass | 322.368 g·mol−1 |
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It is the active (R)-enantiomer of the formerly clinically used stimulant-like drug mesocarb (MLR-1017; brand name Sydnocarb).[1][2][3]
Pharmacology
Mesocarb is known to be a highly selective DRI.[2] However, in 2021, it was discovered that mesocarb is not a conventional DRI but acts as a dopamine transporter (DAT) allosteric modulator or non-competitive inhibitor.[4][5][6]
In accordance with its nature as an atypical DAT blocker, the drug exhibits atypical effects compared to conventional DRIs.[4][5][6][2] For example, mesocarb shows greater antiparkinsonian activity in animals compared to other DRIs.[2]
Mesocarb has wakefulness-promoting effects in animals.[2][7] Armesocarb, as the active enantiomer of mesocarb, shows greater therapeutic potency than the racemic form in animals.[1][2][3] In contrast, the (S)- or D-enantiomer of mesocarb is virtually inactive in animal behavioral tests.[3]
History
Armesocarb was first described in the scientific literature as an enantiopure compound by 2005 and again in 2017.[3][2]
Clinical studies
As of April 2023, armesocarb is undergoing phase 1 clinical trials for Parkinson's disease and is in preclinical development for sleep disorders.[1] The latter indication may specifically target excessive daytime sleepiness (EDS) in people with Parkinson's disease.[2] Armesocarb is also in development for the treatment of levodopa-induced dyskinesia.[8][2]