Differential solubilities in subregions of the membrane: a nonsteric mechanism of drug specificity.
We studied the effect of four volatile anesthetics and convulsants on the GABA- and glutamate-induced conductance change in crab muscle. The intensity of drug action correlated with the solubility parameter (delta) values of the four drugs. Thus, the higher that value was for a given drug, the stronger was its effect on the glutamate response but the weaker was it on the response to gamma-aminobutyric acid (GABA). We suggest that different gating molecules are housed in specific subregions of the membrane, each characterized by a particular value of the solubility parameter. The differential distribution of drugs in these subregions may be a nonsteric mechanism for drug specificity.
D000777:Anesthetics / Q000494:pharmacology*; D000818:Animals; D001001:Anura; D003386:Brachyura; D003292:Convulsants / Q000494:pharmacology*; D066298:In Vitro Techniques; D008566:Membranes / Q000187:drug effects* / Q000378:metabolism; D009431:Neural Conduction / Q000187:drug effects*; D011955:Receptors, Drug / Q000187:drug effects; D012995:Solubility; D013569:Synapses / Q000187:drug effects
D000777:Anesthetics; D003292:Convulsants; D011955:Receptors, Drug