Delving into the Latest Updates on A-794282 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

mGluR1

Mechanism

mGluR1 antagonists(Metabotropic glutamate receptor 1 antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Pain, Postoperative

Originator Organization

Abbott Laboratories

Active Organization-

Inactive Organization

Abbott Laboratories

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC19H18N4OS

InChIKeyVCUKKMIXURRDKL-UHFFFAOYSA-N

CAS Registry869802-44-8

Activation of metabotropic glutamate (mGlu) receptors has previously been shown to play a role in inflammatory or neuropathic pain states. However, the role of mGlu type 1 receptors in post-operative pain remains to be investigated. In the present study, effects of potent and selective mGlu1 receptor antagonists A-841720, A-794282, A-794278, and A-850002 were evaluated in a skin incision-induced post-operative pain model in rats. Post-operative pain was examined 2 h following surgery using weight-bearing difference between injured and uninjured paws as a measure of spontaneous pain. In this model, A-841720, A-794282, A-794278, and A-850002 induced significant attenuation of spontaneous post-operative pain behavior, with ED50s of 10, 50, 50, and 65 micromol/kg i.p., respectively. Depending on the compound, significant motor side effects were also observed at 3 to 10 fold higher doses. These results support the notion that mGlu1 receptor activation plays a significant role in nociceptive transmission in post-operative pain, though motor impairment may be a limiting factor in developing mGlu1 receptor antagonists as novel analgesics.

100 Deals associated with A-794282

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