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Toxicol Lett. 1998 Nov 23;100-101:139-47.

Approaches to proving there are general anesthetic sites on ligand gated ion channels.

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Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.


(1) There are at least two broad classes of general anesthetic action on the anesthetic-sensitive ligand gated superfamily of ion channels. (2) First, some channels may be inhibited upon opening. Pharmacology, kinetics and site directed mutagenesis all suggest that inhibition is mediated by a site on the acetylcholine receptor probably located in the channel lumen. (3) Second, the agonist's concentration response curve may be shifted to the left without affecting the maximum response. (4) This effect does not saturate with anesthetic concentration and might involve partial occupancy of many low affinity sites, mechanism consistent with the observation that the conformation changes accompanying channel gating involve most structural features of the receptor and its surrounding environment.

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