Spin labeled acetylcholine analogs: studies of cholinergic receptor

G. M. Rosen, M. B. Abou Donia, J. Z. Yeh, D. B. Menzel

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Some spin labeled acetylcholine analogs, in which the number of methylene groups between the quaternary nitrogen and the ether oxygen ranged between 1-5, were synthesized to study drug interactions with acetylcholine receptors. None of the compounds tested, with the exception of the one that contained 2 methylene groups (SL 2) had any cholinergic activity. SL 2 was not capable of producing any nicotinic cholinomimetic activity. On the other hand it proved to have a very weak nicotinic cholinolytic activity on the receptors of the frog sartorius muscle. This compound exhibited strong antagonism against muscarinic receptors of the isolated frog heart. The muscarinic cholinolytic action of the spin label ACh analog is discussed in terms of the molecular perturbation theory of drug action.

Original languageEnglish (US)
Pages (from-to)317-329
Number of pages13
JournalResearch Communications in Chemical Pathology and Pharmacology
Volume12
Issue number2
StatePublished - Dec 1 1975

ASJC Scopus subject areas

  • Pathology and Forensic Medicine
  • Toxicology
  • Pharmacology
  • Pharmacology, Toxicology and Pharmaceutics(all)

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