ArticleBritish journal of pharmacology1994
Beta 1- and beta 2-adrenoceptor antagonist activities of ICI-215001, a putative beta 3-adrenoceptor agonist.
Article in British journal of pharmacology, 1994. 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, 28 citations in OpenAlex.
- Cinnamic acid lowers blood pressure and reverses vascular endothelial dysfunction in rats.Journal of food and drug analysis · 2024Article
- Synthesis, docking study and β-adrenoceptor activity of some new oxime ether derivatives.Molecules (Basel, Switzerland) · 2014Article
- β(3) Receptors: Role in Cardiometabolic Disorders.Therapeutic advances in endocrinology and metabolism · 2011Article
- Epinephrine enhances the sensitivity of rat vagal chemosensitive neurons: role of beta3-adrenoceptor.Journal of applied physiology (Bethesda, Md. : 1985) · 2007Article
- Tools to study beta3-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2007Review
- Beta 1-, beta 2- and atypical beta-adrenoceptor-mediated relaxation in rat isolated aorta.British journal of pharmacology · 2000Article
- Effects on energy utilization of a beta3-adrenergic agonist in rats fed on a cafeteria diet.Eating and weight disorders : EWD · 1997Article
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The present study was undertaken to characterize the beta 3-adrenoceptor agonist activity of ICI-215001 and to determine whether it exhibits additional activities on beta 1- and beta 2-adrenoceptors in isolated spontaneously beating atrium, trachea and ileum of guinea-pig. 2. In guinea-pig atrium, isoprenaline, a non-selective beta-adrenoceptor agonist, caused concentration-dependent, positive chronotropic effects that were inhibited by atenolol, a selective beta 1-antagonist. ICI-215001 also competitively antagonized the increase in heart rate caused by isoprenaline. 3. ICI-215001 exhibited low intrinsic activity at increasing the beating rate of atrium and no activity on resting or induced tone of tracheal strips. 4. In strips of guinea-pig trachea, contracted submaximally with carbachol, isoprenaline, caused concentration-dependent relaxations. Both ICI-118551, a selective beta 2-adrenoceptor antagonist, and ICI-215001 competitively inhibited the relaxations caused by isoprenaline. 5. In isolated strips of guinea-pig ileum longitudinal smooth muscle contracted with histamine, isoprenaline and ICI-215001 caused relaxations which were inhibited by alprenolol, a beta-adrenoceptor antagonist with modest affinity for beta 3-adrenoceptors, but were resistant to ICI-118551 and atenolol. 6. These results indicate that ICI-215001 exhibits beta 3-adrenoceptor agonist activity as demonstrated by relaxations mediated via atypical beta-adrenoceptors in the longitudinal smooth muscle of guinea-pig ileum. Further, the studies demonstrate that ICI-215001 can act as an antagonist at beta 1- and beta 2-adrenoceptors in situations where its intrinsic agonist activity is low.
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