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Central GABA‐ergic systems and analgesia
Author(s) -
Defeudis F. V.
Publication year - 1983
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430030102
Subject(s) - opiate , pharmacology , morphine , (+) naloxone , gaba transaminase , nipecotic acid , analgesic , chemistry , gaba receptor antagonist , salicylamide , central nervous system , antagonist , medicine , neurotransmitter , biochemistry , enzyme , glutamate decarboxylase , receptor , bicuculline , organic chemistry
Recent studies regarding the relationship between GABA‐ergic systems and analgesia have been reviewed and analyzed. It seems evident that central GABA‐ergic systems are involved in opiate‐mediated analgesia since oral or parenteral administration of agents that elicit increases in GABA content of the CNS can enhance the actions of opiates (e.g., morphine). Also, oral or parenteral administration of GABA‐agonists (e.g., 4,5,6,7‐tetrahydroisoxazolo[5,4‐c]‐pyridin‐3‐ol; THIP), inhibitors of GABA‐α‐oxoglutarate transaminase (e.g., γ‐vinyl‐GABA), or GABA uptake inhibitors (e.g., nipecotic acid ethyl ester) can produce analgesia. As the analgesia produced by agents that enhance central GABA‐ergic mechanisms is not reversed by naloxone, its further study might lead to the development of centrally active analgesic drugs that do not produce physical dependence/tolerance in man.