Influence of halothane on the interactions of serotonin1A and adenosine A1 receptors with G proteins in rat brain membranes.
The influence of halothane on the interactions of 5-HT1A and adenosine A1 receptors with G proteins was determined by monitoring the guanine nucleotide sensitivity of agonist binding to these receptors. Halothane inhibited the binding of radiolabeled agonists to 5-HT1A and adenosine A1 receptors by up to 30%, but only at concentrations considerably greater than those necessary for the maintenance of the anesthetic state. The sensitivity of high-affinity agonist binding to a guanine nucleotide (guanylyl-5'-imidodiphosphate) was not affected by halothane, indicating no disruption of receptor-G protein coupling. Thus, it appears that the ability of halothane to disrupt receptor-mediated signal transduction by interference with receptor-G protein interactions is receptor specific.
Martin
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DC
Department of Anesthesiology, Medical College of Georgia, Augusta 30912-2700.
Dennison
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Introna
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Aronstam
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D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000241:Adenosine / Q000031:analogs & derivatives / Q000378:metabolism; D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002462:Cell Membrane / Q000187:drug effects; D019204:GTP-Binding Proteins / Q000378:metabolism*; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology; D006221:Halothane / Q000494:pharmacology*; D006624:Hippocampus / Q000187:drug effects; D051381:Rats; D011983:Receptors, Purinergic / Q000187:drug effects* / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D013764:Tetrahydronaphthalenes / Q000378:metabolism; D014316:Tritium
D011983:Receptors, Purinergic; D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; D014316:Tritium; D006165:Guanylyl Imidodiphosphate; C027513:N(6)-cyclohexyladenosine; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D019204:GTP-Binding Proteins; D000241:Adenosine; D006221:Halothane