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. 1988 Jun;8(2):181–191. doi: 10.1007/BF00711244

Two affinity states of M1 muscarine receptors

Lincoln T Potter 1, Cynthia A Ferrendelli 1, Helene E Hanchett 1
PMCID: PMC11567210  PMID: 3409266

Abstract

  1. The binding of oxotremorine-M to M1 muscarine receptors was examined by measuring competition between the agonist and3H-pirenzepine, using rabbit hippocampal membranes suspended in 20 mM Tris buffer containing 1 mM Mn2+.

  2. Both ligands interacted with a single class of receptors. The receptors could assume two affinity states for oxotremorine-M, with equal numbers of high-affinity (K H) and low-affinity (K L) sites.

  3. K H interconverted reversibly toK L in the absence of divalent cations and interconverted reversibly to a state similar toK L in the presence of guanyl 5′-yl imidodiphosphate.

  4. The results are compatible with a model in which a model in which a pair of receptor molecules can be stabilized by a guanine nucleotide-binding “G protein” and have one site each ofK H andK L affinity.

Key words: muscarinic receptors, pirenzepine, acetylcholine, oxotremorine-M, manganese

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