Partial agonists at guinea-pig atrial β-adrenoceptors display relaxation responses in the guinea-pig ileum independent of β-adrenoceptor stimulation

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Abstract

1. 1. The β-adrenoceptor mediated responses of oxyfedrine, ritodrine, tazolol, prenalterol, salbutamol and carteolol were examined on guinea-pig left and right atrial and ileal preparations. 2. 2. All agonists tested in left and right atrial preparations were partial agonists relative to isoprenaline. 3. 3. All agonists with the exception of salbutamol, which appeared a full agonist, produced relaxation responses significantly greater than isoprenaline in ileal preparations. 4. 4. The response to ritodrine in the ileum was not influenced by practolol, in a concentration which antagonized the responses of ritodrine in the right atria. 5. 5. The response of the ileum to β-adrenoceptor antagonists of varying lipophyllicity was examined. Propranolol and pindolol both produced relaxation responses relative to their lipophyllicities. No relaxation was observed to atenolol, which exhibits very low lipophyllicity. 6. 6. It is concluded that β-adrenoceptor agonists exhibit a substantial relaxation of guinea-pig ileum that is independent of β-adrenoceptor stimulation. © 1987.

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Grassby, P. F., & Broadley, K. J. (1987). Partial agonists at guinea-pig atrial β-adrenoceptors display relaxation responses in the guinea-pig ileum independent of β-adrenoceptor stimulation. General Pharmacology, 18(1), 25–31. https://doi.org/10.1016/0306-3623(87)90164-9

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