Ionic regulation of antagonist binding to the human muscarinic cholinergic receptor of caudate nucleus

Gary D. Tollefson, Susan Senogles, William H. Frey

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

In this in vitro study we investigated the effects of a variety of cations on binding of the cholinergic antagonist, (3H)-quinuclidinyl benzilate, to the human caudate. Physiologic sodium concentrations induced a state of positive cooperativity upon the human muscarinic cholinergic receptor (nHill=1.41). Lithium at therapeutic equivalency (1 mM) was unique in increasing the dissociation constant (KD) for this antagonist from 35.9 to 72.4 pM. This implies a lithium-induced cholinomimetic effect at the human muscarinic receptor consistent with reports of the reversal of mania by physostigmine. These findings are also relevant to previous cholinergic receptor studies in which various cations have been employed.

Original languageEnglish (US)
Pages (from-to)275-283
Number of pages9
JournalJournal of Psychiatric Research
Volume17
Issue number3
DOIs
StatePublished - Jan 1 1982

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Caudate Nucleus
Cholinergic Receptors
Muscarinic Receptors
Lithium
Cations
Dissociative Disorders
Quinuclidinyl Benzilate
Therapeutic Equivalency
Physostigmine
Cholinergic Antagonists
Bipolar Disorder
Cholinergic Agents
Sodium

All Science Journal Classification (ASJC) codes

  • Psychiatry and Mental health
  • Biological Psychiatry

Cite this

Ionic regulation of antagonist binding to the human muscarinic cholinergic receptor of caudate nucleus. / Tollefson, Gary D.; Senogles, Susan; Frey, William H.

In: Journal of Psychiatric Research, Vol. 17, No. 3, 01.01.1982, p. 275-283.

Research output: Contribution to journalArticle

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