Gamma-aminobutyric acid enhancement of halothane binding in rat cerebellum.
Quantitative autoradiography of 14C-halothane direct photolabeled rat cerebellum sections was performed in the presence of increasing concentrations of gamma-aminobutyric acid (GABA) or glutamate to test the hypothesis that a coupled binding equilibrium between the anesthetic and neurotransmitter exists. The results show that halothane binding was enhanced in the presence of GABA by approximately 50% in the molecular layer and to a lesser extent in the granular layer, with no change in the myelin layer. Glutamate, however, did not enhance halothane binding in any layer. These data confirm the presence of coupling, and thus suggest a direct interaction of halothane with a GABA binding protein.
Eckenhoff
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Department of Anesthesia, University of Pennsylvania Medical Center, 3400 Spruce Street, Philadelphia, PA 19104-4283, USA. meckenho@mail.med.upenn.edu
Eckenhoff
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D000818:Animals; D001665:Binding Sites / Q000187:drug effects / Q000502:physiology; D001667:Binding, Competitive / Q000187:drug effects / Q000502:physiology; D002250:Carbon Radioisotopes; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D002525:Cerebellar Cortex / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism*; D004347:Drug Interactions / Q000502:physiology*; D018698:Glutamic Acid / Q000378:metabolism / Q000494:pharmacology*; D006221:Halothane / Q000819:agonists* / Q000494:pharmacology*; D008565:Membrane Proteins / Q000187:drug effects / Q000378:metabolism; D009474:Neurons / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism*; D010777:Photochemistry; D011869:Radioligand Assay; D051381:Rats; D005680:gamma-Aminobutyric Acid / Q000378:metabolism / Q000494:pharmacology*
D002250:Carbon Radioisotopes; D008565:Membrane Proteins; D018698:Glutamic Acid; D005680:gamma-Aminobutyric Acid; D006221:Halothane