Identification of binding sites contributing to volatile anesthetic effects on GABA type A receptors

What is it about?

General anesthetics revolutionized modern medicine, allowing patients to undergo undreamed-of procedures without remembering or feeling pain. However much of how these drugs do what they do remains a mystery, particularly for the inhaled anesthetics. In our study we employ anesthetic analogs that enable the direct identification of binding sites within protein targets. We determined the binding sites for two common inhaled anesthetics, isoflurane and sevoflurane, within two types of GABAA receptors, canonical general anesthetic targets responsible for depression of the nervous system. These results gives new insight into the complexity of volatile anesthetic action, as well as a structural roadmap for further mechanistic investigation.

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