Studies on muscarinic binding sites in human brain identified with [3H]pirenzepine

S. C. Lin, K. C. Olson, H. Okazaki, E. Richelson

Research output: Contribution to journalArticle

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Abstract

Pirenzepine, a potent antimuscarinic agent with apparent selectivity for a subtype (M1) of muscarinic receptors, was used in tritiated form to characterize its binding to human brain tissue. Specific [3H]pirenzepine binding showed rapid association and dissociation. From kinetic and competitive binding experiments, its K(D) was 5.5 nM and 9 nM, respectively. Regional distribution of [3H]pirenzepine binding determined in parallel with [3H]quinuclidinyl benzilate binding, a nonselective muscarinic antagonist, indicated a significant correlation for the maximum number of binding sites for the two radio-ligands in 13 brain regions, with the highest amount of binding for each in the putamen and the least in the cerebellum. Binding for [3H]pirenzepine averaged 57% of that for [3H]quinuclidinyl benzilate, with a range of 20% (cerebellum) to 77% (frontal cortex). Most antidepressants and neuroleptics tested had affinities for [3H]pirenzepine binding sites that were not significantly different from their previously reported values obtained with the use of [3H]quinuclidinyl benzilate.

Original languageEnglish (US)
Pages (from-to)274-279
Number of pages6
JournalJournal of Neurochemistry
Volume46
Issue number1
StatePublished - 1986

Fingerprint

Pirenzepine
Cholinergic Agents
Quinuclidinyl Benzilate
Brain
Binding Sites
Muscarinic Antagonists
Cerebellum
Muscarinic M1 Receptors
Competitive Binding
Putamen
Frontal Lobe
Radio
Antidepressive Agents
Antipsychotic Agents
Association reactions
Tissue
Ligands
Kinetics
Experiments

ASJC Scopus subject areas

  • Biochemistry
  • Cellular and Molecular Neuroscience

Cite this

Lin, S. C., Olson, K. C., Okazaki, H., & Richelson, E. (1986). Studies on muscarinic binding sites in human brain identified with [3H]pirenzepine. Journal of Neurochemistry, 46(1), 274-279.

Studies on muscarinic binding sites in human brain identified with [3H]pirenzepine. / Lin, S. C.; Olson, K. C.; Okazaki, H.; Richelson, E.

In: Journal of Neurochemistry, Vol. 46, No. 1, 1986, p. 274-279.

Research output: Contribution to journalArticle

Lin, SC, Olson, KC, Okazaki, H & Richelson, E 1986, 'Studies on muscarinic binding sites in human brain identified with [3H]pirenzepine', Journal of Neurochemistry, vol. 46, no. 1, pp. 274-279.
Lin, S. C. ; Olson, K. C. ; Okazaki, H. ; Richelson, E. / Studies on muscarinic binding sites in human brain identified with [3H]pirenzepine. In: Journal of Neurochemistry. 1986 ; Vol. 46, No. 1. pp. 274-279.
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