ArticleBritish journal of pharmacology2008
Characterization of the alpha1-adrenoceptor subtype mediating contractions of the pig internal anal sphincter.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- The Sphincter of O'Beirne - Part 1: Study of 18 Normal Subjects.Digestive diseases and sciences · 2021Article
- The Sphincter of O'Beirne-Part 2: Report of a Case of Chronic Constipation with Autonomous Dyssynergia.Digestive diseases and sciences · 2021Article
- Control of Motility in the Internal Anal Sphincter.Journal of neurogastroenterology and motility · 2019Article
- Three Gaseous Neurotransmitters, Nitric oxide, Carbon Monoxide, and Hydrogen Sulfide, Are Involved in the Neurogenic Relaxation Responses of the Porcine Internal Anal Sphincter.Journal of neurogastroenterology and motility · 2016Article
- Investigation of the distribution and function of alpha-adrenoceptors in the sheep isolated internal anal sphincter.British journal of pharmacology · 2010Article
- Subtypes of functional alpha1-adrenoceptor.Cellular and molecular life sciences : CMLS · 2010Review
- Survey of anal sphincter dysfunction using anal manometry in patients with fecal incontinence: a possible guide to therapy.Annals of gastroenterologyArticle
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Authors and funding
3 authors.
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Abstract
background and purposeThe internal anal sphincter has been shown to contract in response to alpha1-adrenoceptor stimulation and therefore alpha1-adrenoceptor agonists may be useful in treating faecal incontinence. This study characterizes the alpha1-adrenoceptor subtype responsible for mediating contraction of the internal anal sphincter of the pig. EXPERIMENTAL APPROACH: The potency of agonists and the affinities of several receptor subtype selective antagonists were determined on smooth muscle strips for the pig internal anal sphincter. Cumulative concentration-response curves were performed using phenylephrine and noradrenaline. KEY
resultsThe potency of the alpha1A-adrenoceptor selective agonist A61603 (pEC50=7.79+/-0.04) was 158-fold greater than that for noradrenaline (pEC50=5.59+/-0.02). Phenylephrine (pEC50=5.99+/-0.05) was 2.5-fold more potent than noradrenaline. The alpha1D-adrenoceptor selective antagonist BMY7378 caused rightward shifts of the concentration-response curves to phenylephrine and noradrenaline, yielding low affinity estimates of 6.59+/-0.15 and 6.33+/-0.13, respectively. Relatively high affinity estimates were obtained for the alpha1A-adrenoceptor selective antagonists, RS100329 (9.01+/-0.14 and 9.06+/-0.22 with phenylephrine and noradrenaline, respectively) and 5-methylurapidil (8.51+/-0.10 and 8.31+/-0.10, respectively). Prazosin antagonized responses of the sphincter to phenylephrine and noradrenaline, yielding mean affinity estimates of 8.58+/-0.10 and 8.15+/-0.08, respectively. The Schild slope for prazosin with phenylephrine was equal to unity (1.01+/-0.24), however the Schild slope using noradrenaline was significantly less than unity (0.50+/-0.11, P<0.05). CONCLUSION AND IMPLICATIONS: The results suggest that contraction of circular smooth muscle from the pig internal anal sphincter is mediated via a population of adrenoceptors with the pharmacological characteristics of the alpha1A/L-adrenoceptor, most probably the alpha1L-adrenoceptor form of this receptor.
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