In vitro activity of RO363, a beta1-adrenoceptor selective agonist

British Journal of Pharmacology
D IakovidisC Raper


1 The beta-adrenoceptor stimulant effects of RO363 and (--)-isoprenaline have been compared in a variety of isolated tissue preparations. 2 RO363 is approximately half as potent as (--)-isoprenaline in tissues where actions are due to beta1-receptor activation (guinea-pig atrial and ileal preparations and ventricular strips from the rabbit, rat and guinea-pig. 3 In uterine and lung strip preparations from the guinea-pig, where responses are due to beta2-receptor stimulation. RO363 is 100 to 350 times less active than (--)-isoprenaline and has a low intrinsic activity. 4 In spontaneously contracted tracheal preparations from the guinea-pig, RO363 is a full agonist and is approximately half as potent as (--)-isoprenaline. These effects of RO363 are due to the activation of a population of beta1-receptors in the tissue since RO363 and (--)-isoprenaline have the same relative potencies in trachea, cardiac and ileal preparations. In addition the Kb values for practolol are similar in all these preparations when RO363 is used as the agonist. 5 The results show that RO363 is a potent and highly selective beta1-receptor agonist.


Dec 1, 1977·Journal of Medicinal Chemistry·G LeclercJ Schwartz
Nov 10, 1977·Naunyn-Schmiedeberg's Archives of Pharmacology·E CarlssonB Tångstrand
Nov 15, 1978·European Journal of Pharmacology·C RaperD Iakovidis
Feb 15, 1979·European Journal of Pharmacology·P K SieglR F Orzechowski
Nov 1, 1975·Clinical and Experimental Pharmacology & Physiology·S R O'Donnell, J C Wanstall
Jan 1, 1975·The Journal of Pharmacy and Pharmacology·E J Cornish, R C Miller
Jul 1, 1978·Clinical and Experimental Pharmacology & Physiology·G S KehH Dowd
Mar 1, 1973·European Journal of Pharmacology·E J Mylecharane, C Raper
Jan 1, 1974·Advances in Cardiology·B AbladE Hultberg
Oct 1, 1972·British Journal of Pharmacology·G M Drew, G P Levy
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD


Jul 1, 1983·Naunyn-Schmiedeberg's Archives of Pharmacology·C MaccarroneC Raper
Oct 1, 1982·European Journal of Clinical Pharmacology·C G Löfdahl, N Svedmyr
Nov 1, 1985·Naunyn-Schmiedeberg's Archives of Pharmacology·P MolenaarC Raper
Dec 10, 1985·European Journal of Pharmacology·G A McPhersonC Raper
Jul 1, 1994·General Pharmacology·B N WuI J Chen
May 1, 1987·Clinical and Experimental Pharmacology & Physiology·C Raper
Jul 1, 1987·Clinical and Experimental Pharmacology & Physiology·J N PennefatherJ A Leedham
Jan 1, 1995·Pharmacology & Toxicology·B Waldeck
Oct 1, 1987·The American Review of Respiratory Disease·J ZaagsmaV Veenstra
May 1, 1985·British Journal of Pharmacology·E MaltaC Raper
May 1, 1983·British Journal of Pharmacology·R G GoldieJ L Wale
Oct 1, 1985·British Journal of Pharmacology·C Advenier, J L Freslon
Jul 1, 1986·British Journal of Pharmacology·G A Bentley, J Starr
Jul 1, 1983·Medicinal Research Reviews·J A Bristol, D B Evans
Feb 1, 1985·British Journal of Pharmacology·M L Hartley, J N Pennefather
Jun 1, 1981·Journal of Autonomic Pharmacology·S A Doggrell, L Vincent
Sep 1, 1983·British Journal of Pharmacology·J F BertramJ W Paterson

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