The cloned murine M1 muscarinic receptor is associated with the hydrolysis of phosphatidylinositols in transfected murine B82 cells

Josephine Lai, Lin Mei, William R. Roeske, Fu Zon Chung, Henry I. Yamamura, J. Craig Venter

Research output: Contribution to journalArticlepeer-review

47 Scopus citations

Abstract

A rat genomic DNA clone was isolated by its homology with a conserved primary sequence among the mammalian and avian beta adrenergic and procine muscarinic receptors. A gene identified in this clone was highly homologous to the rat M1 muscarinic receptor. Stable expression of this gene was achieved in an established murine fibroblast cell line, B82. The gene product exhibits M1 type muscarinic receptor characteristics, as it has high affinity for PZ but low affinity for AF-DX 116. Carbachol stimulated the hydrolysis of phosphatidylinositols in the transfected cells. Pirenzepine had a more potent inhibitory effect on this response than AF-DX 116 since their functional inhibition constants were 13 nM and 480 nM, respectively, which is consistent with an M1 pharmacological profile. These data suggest that the M1 muscarinic receptor encoded by the gene is coupled to the hydrolysis of phosphatidylinositols after transfecting this gene into the B82 cells.

Original languageEnglish (US)
Pages (from-to)2489-2502
Number of pages14
JournalLife sciences
Volume42
Issue number24
DOIs
StatePublished - 1988

ASJC Scopus subject areas

  • General Pharmacology, Toxicology and Pharmaceutics
  • General Biochemistry, Genetics and Molecular Biology

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