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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Responses to the beta 2-selective agonist procaterol of vascular and atrial preparations with different functional beta-adrenoceptor populations.

Relaxant responses to the beta-adrenoceptor agonist, procaterol, have been examined on preparations of guinea-pig pulmonary artery (beta 2-adrenoceptors only), rat and rabbit pulmonary artery and rat aorta (beta 2 greater than beta 1), and these responses have been compared with responses of dog left circumflex coronary artery (beta 1 only). Low concentrations of procaterol (3 nM to 100 nM) relaxed KC1-contracted preparations of rat aorta and pulmonary artery from rat, rabbit and guinea-pig whereas high concentrations (greater than 1 microM) were required to relax preparations of the dog left circumflex coronary artery. The dissociation constant (KP value) for procaterol on beta 1-adrenoceptors was 4.9 microM (determined on dog coronary artery) and on beta 2-adrenoceptors was 0.008 microM (rabbit pulmonary artery). Procaterol therefore had a beta 2:beta 1 selectivity value of 612. KP values obtained on guinea-pig atria for procaterol, on which the concentration-response curve was biphasic, confirmed that both beta 2- and beta 1-adrenoceptors mediate responses of this tissue. The KP values were 0.009 microM (data from the first phase of the control concentration-response curve) and 3.5 microM (data from the concentration-response curve in the presence of the beta 2-selective antagonist, ICI 118,551, 10 nM). Data obtained on rat atria indicated that chronotropic responses of preparations from some rats, but not others, involved a minor population of beta 2-adrenoceptors, but the beta 2-adrenoceptors, when present, were less important than in guinea-pig atria.(ABSTRACT TRUNCATED AT 250 WORDS)[1]


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