ArticleBritish journal of pharmacology1995
Characterization and localization of atypical beta-adrenoceptors in rat ileum.
Article in British journal of pharmacology, 1995. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 27 citations in OpenAlex.
- Adrenoceptors: Receptors, Ligands and Their Clinical Uses, Molecular Pharmacology and Assays.Handbook of experimental pharmacology · 2024Review
- β(3) Receptors: Role in Cardiometabolic Disorders.Therapeutic advances in endocrinology and metabolism · 2011Article
- SAR150640, a selective beta3-adrenoceptor agonist, prevents human myometrial remodelling and activation of matrix metalloproteinase in an in vitro model of chorioamnionitis.British journal of pharmacology · 2010Article
- The rush to adrenaline: drugs in sport acting on the beta-adrenergic system.British journal of pharmacology · 2008Review
- Is the beta3-adrenoceptor (ADRB3) a potential target for uterorelaxant drugs?BMC pregnancy and childbirth · 2007Review
- beta(1)-Adrenoceptors compensate for beta(3)-adrenoceptors in ileum from beta(3)-adrenoceptor knock-out mice.British journal of pharmacology · 2001Article
- Functional, biochemical and molecular biological evidence for a possible beta(3)-adrenoceptor in human near-term myometrium.British journal of pharmacology · 2000Article
- beta(3)-adrenoceptor regulation and relaxation responses in mouse ileum.British journal of pharmacology · 2000Article
- Characterization of beta-adrenoceptor mediated smooth muscle relaxation and the detection of mRNA for beta1-, beta2- and beta3-adrenoceptors in rat ileum.British journal of pharmacology · 1999Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
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 predominantly in the longitudinal and circular smooth muscle layers. 6. This study identifies an (-)-[125I]-CYP binding site in rat ileum that is resistant to blockade by propranolol (0.1 microM), is located predominantly in the mucosa, shows resistance to downregulation by isoprenaline and has binding characteristics of the atypical beta-AR.
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