Irena Kosmowska

RespireRx Pharmaceuticals Inc. Discloses Novel Structural Analogs of its GABAA Receptor Potentiator, KRM-II-81 with Antiseizure Efficacy and Antitremor Effects without Sedation.

Retrieved on: 
Montag, April 3, 2023

Like KRM-II-81, these analogs enhance GABAergic neurotransmission and function as orally-bioavailable anti-seizure agents in the absence of the sedation typically associated with GABA augmentation.

Key Points: 
  • Like KRM-II-81, these analogs enhance GABAergic neurotransmission and function as orally-bioavailable anti-seizure agents in the absence of the sedation typically associated with GABA augmentation.
  • In addition KRM-II-81 is active in relieving acute, chronic, and neuropathic pain in a number of models without developing tolerance or producing sedation.
  • 385:50-61 document the preclinical effects and tolerability of structural analogs of KRM-II-81.
  • In established rat models predicting efficacy in essential tremor and in tremor associated with Parkinson’s Disease, MP-III-024 was an effective anti-tremor compound.