Characterization and localization of atypical β‐adrenoceptors in rat ileum

Susan J. Roberts, Fraser D. Russell, Peter Molenaar, Roger J. Summers

Research output: Contribution to journalArticleResearchpeer-review

Abstract

. 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. . 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 β1 and β‐adrenoceptors (AR) were not detected in these preparations. . (—)‐Isoprenaline infusion (400 μg 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). . Competition for (—)‐[125I]‐CYP binding in the presence of 0.1 μm (—)‐propranolol gave affinity values for CYP, tertatolol, alprenolol, ICI 118551 and CGP 20712A that correspond to known affinities at atypical β‐ARs. Stereoselectivity ratios for tertatolol and alprenolol were low. . 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 β2‐ARs were detected located predominantly in the longitudinal and circular smooth muscle layers. . This study identifies an (—)‐[125I]‐CYP binding site in rat ileum that is resistant to blockade by propranolol (0.1 μm), is located predominantly in the mucosa, shows resistance to downregulation by isoprenaline and has binding characteristics of the atypical β‐AR. 1995 British Pharmacological Society

Original languageEnglish
Pages (from-to)2549-2556
Number of pages8
JournalBritish Journal of Pharmacology
Volume116
Issue number6
DOIs
Publication statusPublished - 1 Jan 1995
Externally publishedYes

Keywords

  • (—)‐[I]‐cyanopindolol
  • atypical β‐adrenoceptor
  • autoradiography
  • localization
  • rat ileum
  • regulation
  • β ‐Adrenoceptor

Cite this

Roberts, Susan J. ; Russell, Fraser D. ; Molenaar, Peter ; Summers, Roger J. / Characterization and localization of atypical β‐adrenoceptors in rat ileum. In: British Journal of Pharmacology. 1995 ; Vol. 116, No. 6. pp. 2549-2556.
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abstract = ". 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. . 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 β1 and β‐adrenoceptors (AR) were not detected in these preparations. . (—)‐Isoprenaline infusion (400 μg 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). . Competition for (—)‐[125I]‐CYP binding in the presence of 0.1 μm (—)‐propranolol gave affinity values for CYP, tertatolol, alprenolol, ICI 118551 and CGP 20712A that correspond to known affinities at atypical β‐ARs. Stereoselectivity ratios for tertatolol and alprenolol were low. . 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 β2‐ARs were detected located predominantly in the longitudinal and circular smooth muscle layers. . This study identifies an (—)‐[125I]‐CYP binding site in rat ileum that is resistant to blockade by propranolol (0.1 μm), is located predominantly in the mucosa, shows resistance to downregulation by isoprenaline and has binding characteristics of the atypical β‐AR. 1995 British Pharmacological Society",
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Characterization and localization of atypical β‐adrenoceptors in rat ileum. / Roberts, Susan J.; Russell, Fraser D.; Molenaar, Peter; Summers, Roger J.

In: British Journal of Pharmacology, Vol. 116, No. 6, 01.01.1995, p. 2549-2556.

Research output: Contribution to journalArticleResearchpeer-review

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T1 - Characterization and localization of atypical β‐adrenoceptors in rat ileum

AU - Roberts, Susan J.

AU - Russell, Fraser D.

AU - Molenaar, Peter

AU - Summers, Roger J.

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N2 - . 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. . 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 β1 and β‐adrenoceptors (AR) were not detected in these preparations. . (—)‐Isoprenaline infusion (400 μg 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). . Competition for (—)‐[125I]‐CYP binding in the presence of 0.1 μm (—)‐propranolol gave affinity values for CYP, tertatolol, alprenolol, ICI 118551 and CGP 20712A that correspond to known affinities at atypical β‐ARs. Stereoselectivity ratios for tertatolol and alprenolol were low. . 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 β2‐ARs were detected located predominantly in the longitudinal and circular smooth muscle layers. . This study identifies an (—)‐[125I]‐CYP binding site in rat ileum that is resistant to blockade by propranolol (0.1 μm), is located predominantly in the mucosa, shows resistance to downregulation by isoprenaline and has binding characteristics of the atypical β‐AR. 1995 British Pharmacological Society

AB - . 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. . 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 β1 and β‐adrenoceptors (AR) were not detected in these preparations. . (—)‐Isoprenaline infusion (400 μg 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). . Competition for (—)‐[125I]‐CYP binding in the presence of 0.1 μm (—)‐propranolol gave affinity values for CYP, tertatolol, alprenolol, ICI 118551 and CGP 20712A that correspond to known affinities at atypical β‐ARs. Stereoselectivity ratios for tertatolol and alprenolol were low. . 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 β2‐ARs were detected located predominantly in the longitudinal and circular smooth muscle layers. . This study identifies an (—)‐[125I]‐CYP binding site in rat ileum that is resistant to blockade by propranolol (0.1 μm), is located predominantly in the mucosa, shows resistance to downregulation by isoprenaline and has binding characteristics of the atypical β‐AR. 1995 British Pharmacological Society

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KW - atypical β‐adrenoceptor

KW - autoradiography

KW - localization

KW - rat ileum

KW - regulation

KW - β ‐Adrenoceptor

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