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Evaluation of a new beta adrenoceptor agonist procaterol based on metabolic responses in rats


, : Evaluation of a new beta adrenoceptor agonist procaterol based on metabolic responses in rats. Biochemical Pharmacology 27(21): 2531-2536

I.v. injection of 5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril hydrochloride hemihydrate (procaterol) or isoproterenol into fasted rats caused increases in blood levels of glucose, lactate, free fatty acids (FFA), glycerol, immunoreactive insulin and cAMP. Procaterol-induced alterations of these metabolic parameters, other than FFA, were durable; the increases were observable over a period longer than 2 h, in contrast to a much shorter duration of isoproterenol-induced metabolic changes. These actions of procaterol were antagonized by propranolol, were observed in adrenodemedullated rats, and were enhanced by theophylline. Metabolic changes induced by procaterol might actually be mediated via .beta.-adrenoceptors as well as its pharmacological actions. Procaterol caused hyperlactacidemia at M doses 10-100 times lower than those required for isoproterenol, trimetoquinol or salbutamol. A much higher dose of procaterol was required to increase blood levels of FFA, glycerol and insulin. Butoxamine, a selective .beta.2-adrenoceptor antagonist, antagonized the isoproterenol-induced blood lactate, while practolol, a selective .beta.1-antagonist, effectively inhibited the stimulatory actions of isoproterenol on FFA, glycerol and insulin. Procaterol was a more selective .beta.2-adrenoceptor agonist than isoproterenol or trimetoquinol and was more potent than salbutamol.


Accession: 005395340

PMID: 31885

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