A morpholinocatechol compound (UK42620) with clonidine- and tyramine-like actions.
1. The actions of a morpholinocatechol (UK42620) were studied in rat isolated atria preparations consisting of spontaneously beating left and right atrial pairs. 2. UK42620 produced positive inotropic and chronotropic responses and, in atria that were incubated with [(3)H]-noradrenaline, it also produced a massive increase in the release of radioactivity. 3. These actions of UK42620 were similar to those of tyramine and were blocked by the beta-adrenoceptor antagonist propranolol (0.3 microM) and by the neuronal uptake blocker desipramine (1 microM). 4. In the presence of desipramine, UK42620 but not tyramine produced a decrease in the stimulation-induced efflux of radioactivity that was antagonized by idazoxan. 5. Thus, UK42620 had prejunctional alpha(2)-adrenoceptor activity like that of clonidine- and tyramine-like activity releasing large amounts of noradrenaline.
Thaina
P
P
Department of Pharmacology, University of Melbourne, Parkville, Victoria, Australia.
Nott
M W
MW
Rand
M J
MJ
D018759:Adrenergic Uptake Inhibitors / Q000494:pharmacology; D058647:Adrenergic alpha-2 Receptor Agonists; D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000818:Animals; D002316:Cardiotonic Agents / Q000494:pharmacology*; D002396:Catechols / Q000494:pharmacology*; D003000:Clonidine / Q000494:pharmacology*; D003891:Desipramine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects*; D009025:Morpholines / Q000494:pharmacology*; D009200:Myocardial Contraction / Q000187:drug effects; D011433:Propranolol / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D014439:Tyramine / Q000494:pharmacology*
C455579:2-morpholino-4-catechol; D018759:Adrenergic Uptake Inhibitors; D058647:Adrenergic alpha-2 Receptor Agonists; D000316:Adrenergic alpha-Agonists; D000319:Adrenergic beta-Antagonists; D002316:Cardiotonic Agents; D002396:Catechols; D009025:Morpholines; D011433:Propranolol; D003000:Clonidine; D003891:Desipramine; D014439:Tyramine