Characterization and localization of atypical beta-adrenoceptors in rat ileum

British Journal of Pharmacology
S J RobertsR J Summers

Abstract

1. Homogenate binding studies and receptor autoradiography have been used to examine the binding characteristics and localization of propranolol-resistant (-)-[125I]-cyanopindolol (CYP) binding sites in rat ileum. 2. Saturation studies with (-)-[125I]-CYP and homogenates of rat ileum identified a site with pKD 8.89 +/- 0.08 and Bmax = 50.3 +/- 4.1 fmol mg-1 protein (n = 6). Both beta 1- and beta 2-adrenoceptors (AR) were not detected in these preparations. 3. (-)-Isoprenaline infusion (400 micrograms kg-1 h-1) for 14 days caused no significant change in the density of (-)-[125I]-CYP binding which was 48.9 +/- 12.8 and 40.6 +/- 12.3 fmol mg-1 protein in control and isoprenaline-treated animals respectively (n = 6) (P = 0.97). 4. Competition for (-)-[125I]-CYP binding in the presence of 0.1 microM (-)-propranolol gave affinity values for CYP, tertatolol, alprenolol, ICI 118551 and CGP 20712A that correspond to known affinities at atypical beta-ARs. Stereoselectivity ratios for tertatolol and alprenolol were low. 5. Autoradiographic localization of propranolol resistant (-)-[125I]-CYP binding showed sites associated with the mucosa and to a lesser extent to the muscularis. A small population of beta 2-ARs were detected located pre...Continue Reading

References

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Citations

Jan 28, 2004·European Journal of Pharmacology·Ben D PoppRoger J Summers
Mar 22, 2000·British Journal of Pharmacology·D S HutchinsonR J Summers
Feb 13, 2001·British Journal of Pharmacology·D S HutchinsonR J Summers
Jul 25, 1998·Alimentary Pharmacology & Therapeutics·A AnthonyA J Wakefield
Jan 1, 1996·British Journal of Pharmacology·B A EvansR J Summers
Sep 29, 1998·The Journal of Pharmacy and Pharmacology·A Díez-SampedroA Barber
Jun 19, 2007·BMC Pregnancy and Childbirth·Marc BardouJohn J Morrison
May 27, 2008·British Journal of Pharmacology·E DavisR J Summers
Feb 25, 2006·The Journal of Comparative Neurology·Yasmin NasserKeith A Sharkey
Feb 28, 2003·The Journal of Pharmacology and Experimental Therapeutics·Sandeep RathiSatish Rattan
Jan 7, 1999·Developmental and Comparative Immunology·S J Jozefowski, B Plytycz

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