Progesterone modulates a neuronal nicotinic acetylcholine receptor.

• DOI: 10.1073/pnas.89.20.9949
• Publication Date: 2006-05-31T12:10:38Z
• Authors: S Valera; M Ballivet; D Bertrand
• Keywords: 0303 health sciences; Binding Sites; info:eu-repo/classification/ddc/540; Brain; In Vitro Techniques; Receptors, Nicotinic; Acetylcholine; Membrane Potentials; Structure-Activity Relationship; Xenopus laevis; 03 medical and health sciences; Cholesterol; Allosteric Regulation; ddc:540; Oocytes; Animals; Point Mutation; info:eu-repo/classification/ddc/612; Testosterone; ddc:612; Ion Channel Gating; Progesterone

The major brain nicotinic acetylcholine receptor is assembled from two subunits termed alpha 4 and n 1. When expressed in Xenopus oocytes, these reconstitute a functional that inhibited by progesterone levels similar to those found serum. In this report, we show the steroid interacts with site located on extracellular part of protein, thus confirming inhibition not due nonspecific perturbation membrane bilayer or activation second messengers. Because does require presence agonist, voltage-independent, alter desensitization, conclude an open channel blocker. addition, competitive inhibitor but may interact binding its effect independent ionic permeability receptor.