The lack of a pronounced preference of prenalterol for the beta-l-adrenoceptor subtype.
The beta-sympathomimetic effect of prenalterol was investigated on the electrically driven left atrium as well as on the tracheal chain of the guinea pig. 1. On the atrium driven at 2 Hz prenalterol caused a positive inotropic effect with a pD2-value of 7.0 +/- 0.08 (N = 4). Compared to isoprenaline (1.0) its intrinsic activity amounted to 0.3. 2. On the tracheal chain prenalterol caused very little relaxation. Its intrinsic activity was virtually negligible when compared with those of fenoterol (1.0) or noradrenaline (1.0); it amounted to 0.07 only. 3. On the atrium the positive inotropic effect of prenalterol vanished after 1 hour of incubation. At this time the concentration-response curve for isoprenaline was shifted dose-dependently to the right. The pD2-value for isoprenaline was significantly diminished (P less than 0.001) by prenalterol, 10(-6)M, from 8.36 to 7.14. 4. Likewise, on the trachea prenalterol caused a pronounced, dose-dependent shift of the concentration-response curves for fenoterol as well as for noradrenaline to the right. 5. The results presented here show that on beta-adrenoceptors of the guinea pig prenalterol is acting like a partial agonist in the left atrium, but as full antagonist in the trachea.
D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000818:Animals; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007545:Isoproterenol / Q000494:pharmacology; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D011217:Practolol / Q000031:analogs & derivatives* / Q000494:pharmacology; D011294:Prenalterol; D011941:Receptors, Adrenergic / Q000187:drug effects*; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D014132:Trachea / Q000187:drug effects
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D011941:Receptors, Adrenergic; D011943:Receptors, Adrenergic, beta; D007545:Isoproterenol; D011294:Prenalterol; D011217:Practolol