Inhibition of human alpha4beta2 neuronal nicotinic acetylcholine receptors by volatile aromatic anesthetics depends on drug hydrophobicity.

Anesthesia and Analgesia
Ken SoltDouglas E Raines

Abstract

Volatile aromatic compounds such as benzene are general anesthetics that cause amnesia, hypnosis, and immobility in response to noxious stimuli when inhaled. Although these compounds are not used clinically, they are frequently found in commercial items such as solvents and household cleaning products and are abused as inhalant drugs. Volatile aromatic anesthetics are useful pharmacological tools for probing the relationship between chemical structure and drug activity at putative general anesthetic targets. Neuronal nicotinic acetylcholine (nACh) receptors are ligand-gated ion channels widely expressed in the brain, which are thought to play important roles in learning and memory. In this study, we tested the hypothesis that aromatic anesthetics reversibly inhibit alpha(4)beta(2) neuronal nACh receptor function and sought to determine the structural correlates of receptor inhibition. Electrophysiological techniques were used to quantify the effects of 8 volatile aromatic anesthetics on currents elicited by 1 mM ACh and mediated by human alpha(4)beta(2) nACh receptors expressed in Xenopus oocytes. All of the volatile aromatic anesthetics used in this study reversibly inhibited alpha(4)beta(2) nACh receptors with IC(50) values r...Continue Reading

References

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Oct 22, 2008·Anesthesia and Analgesia·Takafumi HorishitaR Adron Harris

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Citations

May 28, 2019·Toxicology and Applied Pharmacology·Monserrat Armenta-ReséndizSilvia Lorenia Cruz

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