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Diminished Functional Activity of Newly Synthesized Muscarinic Acetylcholine Receptors in Stably Transfected Y1 Adrenal Cells
Author(s) -
Ikegaya Takayoshi,
Nathanson Neil M.
Publication year - 1993
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1993.tb03265.x
Subject(s) - muscarinic acetylcholine receptor , transfection , acetylcholine , acetylcholine receptor , muscarinic acetylcholine receptor m3 , muscarinic acetylcholine receptor m4 , receptor , muscarinic acetylcholine receptor m2 , muscarinic acetylcholine receptor m1 , muscarinic acetylcholine receptor m5 , endocrinology , chemistry , medicine , neuroscience , biology , biochemistry , gene
We have examined the functional responsiveness of newly synthesized m2 muscarinic acetylcholine receptors in stably transfected Y1 adrenal cells. After inactivation of preexisting receptors with the covalent alkylating antagonist propylbenzilylcholine mustard, the number of cell surface receptors returned to control values over a 3‐h period. After a 3‐h recovery, the cells exhibited diminished sensitivity for muscarinic receptor‐mediated inhibition of adenylyl cyclase activity, with much higher concentrations of agonist being required to elicit a response. The functional sensitivity returned to control values over a 12–18‐h period. The decreased functional activity was not due to a decreased affinity of the newly synthesized receptors for agonist or to a decrease in the levels of inhibitory G proteins in the cells. The results suggest that muscarinic receptors may be synthesized in a form with diminished functional activity. The ability to study the maturation of receptor function in a transfected cell system should allow a combination of biochemical and molecular genetic approaches to analyze the synthesis and functional responsiveness of muscarinic receptors.