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Updated: Aug 15, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
[Pharmacology of an omega receptor agonist]
1Wyeth K. K., 1-10-3 Kyobashi, Chuo-ku, Tokyo 104-0031, Japan. noguchh@wyeth.com
Abstract:
It has been suggested that different BZP (omega) receptor subtypes may mediate distinct behavioral effects of BZP receptor ligands. Several studies demonstrated that omega1 selective compounds are characterized by an increase in slow wave deep sleep with rapid onset of hypnotic action, and by reduced muscle relaxation, amnesic liability or tolerance. On the other hand, it is known that many different subtypes of GABAA receptors exist, based on the fact that many different subtypes can go into assembling GABAA receptors. GABAA receptors with alpha1 subunits may mediate sedative action and perhaps amnesia. Those with alpha2 subunits probably mediate anxiolytic actions. GABAA receptors with alpha3 subunits may regulate various neurotransmitters, and those with alpha5 subunits may also contribute to amnesia. Such discoveries could open up new avenues for drug development.
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