Binding and hydrodynamic properties of muscarinic receptor subtypes solubilized in 3-(3-cholamidopropyl)dimethylammonio-2-hydroxy-1-propanesulfonate

D. R. Poyner, N. J.M. Birdsall, C. Curtis, P. Eveleigh, E. C. Hulme, E. K. Pedder, M. Wheatley

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

The muscarinic receptor form the cerebral cortex, heart, and lacrimal gland can be solubilized in the zwitterionic detergent 3-(3-cholamidopropyl)dimethylammonio-2-hydroxy-1-propane sulfonate (CHAPSO) with retention of high affinity [3H]N-methylscopolamine binding. However, in this detergent there are significant differences in the binding properties of the receptors, compared with those observed in membranes and digitonin solution. Some agents retain a degree of selectivity. In the heart and cortex, agonists can bind with high affinity to a receptor-GTP-binding protein complex. A second, lower affinity, agonist binding state is also present, which resembles a class of sites seen in membranes but not in digitonin solution. The high affinity agonist binding state has been resolved from the lower affinity state on sucrose density gradient contrifugation. Hydrodynamic analysis suggests that the high affinity state is approximately 110,000 Da larger than the lower affinity state. The binding properties of the receptor in CHAPSO can be altered to those seen in digitonin by exchanging detergents after CHAPSO solubilization.

Original languageEnglish
Pages (from-to)420-429
Number of pages10
JournalMolecular Pharmacology
Volume36
Issue number3
Publication statusPublished - 26 Oct 1989
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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