Effect of pertussis toxin on the heart acetylcholine muscarinic receptor affinity

European Journal of Pharmacology
J L BoyerJ A García-Sáinz

Abstract

The effect of pertussis toxin on the affinity for agonists and antagonists of the heart muscarine acetylcholine receptor was studied using the radiolabeled antagonist [3H]quinuclidinyl benzylate ([3H]QNB). In cardiac membranes from control rats the displacement of [3H]QNB by carbachol was consistent with two classes of binding sites, kDH 25 +/- 10 nM and kDL 3,006 +/- 869 nM. The proportion of sites in the high and low affinity state for agonists was 55 and 45% respectively. In the presence of 100 microM guanyl-5'-yl imidodiphosphate (Gpp(NH)p), only the low affinity state for agonists was observed (kDL 3,804 +/- 759 nM). In cardiac membranes from pertussis toxin-treated rats, two classes of binding sites with affinities similar to those seen in the controls were also observed in the absence of guanine nucleotide (kDs 39 +/- 12 and 3,315 +/- 845 nM) but the proportion of sites were 20 and 80% for high and low affinity respectively. Gpp(NH)p shifted the remaining 20% of sites from the high affinity to the low affinity state (KD 4,093 +/- 744 nM). The receptor KD for antagonists was decreased by pretreatment with pertussis toxin from 83 +/- 7 to 56 +/- 5 pM (P less than 0.01); Gpp(NH)p induced a further change in the affinity for...Continue Reading

References

Apr 27, 1979·Biochemical and Biophysical Research Communications·C P BerrieE C Hulme
Jun 1, 1979·European Journal of Pharmacology·L B RosenbergerH I Yamamura
Apr 30, 1985·Biochemical and Biophysical Research Communications·C C MalbonD C Watkins
Jan 14, 1986·Biochemical and Biophysical Research Communications·J L BoyerJ A García-Sáinz
Jan 1, 1980·Annual Review of Biochemistry·E M Ross, A G Gilman
Jan 1, 1984·The Journal of Clinical Investigation·A G Gilman
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Sep 10, 1982·European Journal of Pharmacology·J L BoyerJ A García-Sáinz
Jul 1, 1983·Proceedings of the National Academy of Sciences of the United States of America·J CodinaC R Manclark
Oct 18, 1983·Biochimica Et Biophysica Acta·M A Martínez-Olmedo, J A García-Sáinz
May 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·T Katada, M Ui
Mar 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·E BurgisserR J Lefkowitz

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Citations

Jan 1, 1988·Pharmacology & Therapeutics·F Mitchelson

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