International Journal of Molecular Sciences (Oct 2022)

Allosteric Modulation of Muscarinic Receptors by Cholesterol, Neurosteroids and Neuroactive Steroids

  • Ewa Szczurowska,
  • Eszter Szánti-Pintér,
  • Alena Randáková,
  • Jan Jakubík,
  • Eva Kudova

DOI
https://doi.org/10.3390/ijms232113075
Journal volume & issue
Vol. 23, no. 21
p. 13075

Abstract

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Muscarinic acetylcholine receptors are membrane receptors involved in many physiological processes. Malfunction of muscarinic signaling is a cause of various internal diseases, as well as psychiatric and neurologic conditions. Cholesterol, neurosteroids, neuroactive steroids, and steroid hormones are molecules of steroid origin that, besides having well-known genomic effects, also modulate membrane proteins including muscarinic acetylcholine receptors. Here, we review current knowledge on the allosteric modulation of muscarinic receptors by these steroids. We give a perspective on the research on the non-genomic effects of steroidal compounds on muscarinic receptors and drug development, with an aim to ultimately exploit such knowledge.

Keywords