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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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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]
It is the active (R)-enantiomer of the formerly clinically used stimulant-like drug mesocarb (MLR-1017; brand name Sydnocarb). [1] [2] [3]
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]
Armesocarb was first described in the scientific literature as an enantiopure compound by 2005 and again in 2017. [3] [2]
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]