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    (+)-Borneol alleviates mechanical hyperalgesia in models of chronic inflammatory and neuropathic pain in mice
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    The first edition of The GABA Receptors (Enna, 1983) made no reference to the subtype of GABA receptors now known as GABAC receptors, i.e., receptors for the inhibitory neurotransmitter GABA that are insensitive to the GABAA antagonist, bicuculline, and to the GABAB agonist, baclofen. Bowery (1993), in his chapter on the classification of GABA receptors, reported that the possible existence of bicuculline-insensitive GABA receptors had been considered, e.g., Andrews and Johnston (1979) postulated that "GABA might act at a population of bicuculline-insensitive sites in a folded conformation whereas it acts at bicuculline-sensitive receptors in an extended conformation." Bowery continued, "The idea arose from studies with compounds such as cis-4-aminocrotonic acid that depress neuronal firing but are unaffected by bicuculline. Although this postulate is interesting, a simultaneous activation of these sites by GABA in the presence of bicuculline was never shown. To designate a receptor 'GABA site,' it surely must be activated by GABA. Perhaps under the right conditions GABA may be an agonist at the site."KeywordsPartial AgonistBipolar CellGaba ReceptorHorizontal CellGlycine ReceptorThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
    GABAB receptor
    GABA receptor antagonist
    GABAA-rho receptor
    GABA receptor
    Baclofen
    Laryngeal motoneurons in the nucleus ambiguus were activated antidromically to ipsilateral recurrent nerve stimulation in urethane-chloralose anaesthetized rats. GABAA agonist muscimol and the antagonist bicuculline were applied separately or together with GABA iontophoretically with a multibarrel pipette glued with a recording electrode. The majority of neurons (119/155) which did not respond to the recurrent nerve stimulation exhibited activities mostly related to inspiration. Other 32 neurons were classified as laryngeal motoneurons, according to the criteria. Bicuculline application antagonized GABAA-mediated inhibition while muscimol or GABA reversed this effect significantly. Dose dependent changes were observed for administration of these GABAA-related agents. It can be concluded therefore that laryngeal motoneurons received GABAA-mediated inhibition.
    Muscimol
    GABA receptor antagonist
    Nucleus ambiguus
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    Alterations in a low affinity form of the GABAA receptor were examined with [3H]bicuculline methylchloride in the adult rat following perinatal exposure to diazepam. Perinatal exposure resulted in a significant reduction in [3H]bicuculline binding in the cingulate cortex. A significant decrease in the ability of GABA to displace bound [3H]bicuculline was observed only in the hypothalamus. The results suggest that the effects of perinatal exposure to diazepam are regionally specific and that benzodiazepine receptors and low affinity GABAA receptors are functionally linked during the perinatal period.
    GABA receptor antagonist