Moore P F, Constantine J W, Barth W E
J Pharmacol Exp Ther. 1978 Nov;207(2):410-8.
Pirbuterol, 2-hydroxymethyl-3-hydroxy-6-(1-hydroxy-2-tert-butylaminoethyl)pyridine, is a new beta2 adrenergic agonist bronchodilator. Comparison of the relative potencies of pirbuterol, salbutamol and isoproterenol as relaxants of isolated guinea-pig tracheal muscle and as positive chronotropic agents in isolated guinea-pig atria indicate that the relative selectivity of pirbuterol for pulmonary as opposed to cardiac tissue is 9 times greater than that for salbutamol and some 1500 times greater than that for isoproterenol. Pirbuterol is effective by the oral, intravenous and inhalation routes of administration. In conscious guinea pigs, pirbuterol antagonizes both histamine- and acetylcholine-induced bronchoconstriction and "microshock" anaphylaxis; combinations of pirbuterol and theophylline cause additive effects against histamine-induced bronchoconstriction. In conscious dogs, the cardiovascular effects of pirbuterol are clearly distinguished from those of salbutamol, in that salbutamol causes a more pronounced tachycardia. In anesthetized dogs the cardiovascular effects of pirbuterol and salbutamol are comparable; they are less potent than isoproterenol and have less pronounced although longer lasting effects.
吡布特罗，即2-羟甲基-3-羟基-6-(1-羟基-2-叔丁氨基乙基)吡啶，是一种新型β2肾上腺素能激动剂支气管扩张剂。对吡布特罗、沙丁胺醇和异丙肾上腺素作为离体豚鼠气管肌肉松弛剂以及离体豚鼠心房正性变时剂的相对效价进行比较表明，吡布特罗对肺组织而非心脏组织的相对选择性比沙丁胺醇高9倍，比异丙肾上腺素高约1500倍。吡布特罗通过口服、静脉注射和吸入途径给药均有效。在清醒的豚鼠中，吡布特罗可拮抗组胺和乙酰胆碱引起的支气管收缩以及“微休克”过敏反应；吡布特罗与茶碱联合使用对组胺引起的支气管收缩具有相加作用。在清醒的犬中，吡布特罗的心血管效应与沙丁胺醇明显不同，因为沙丁胺醇会引起更明显的心动过速。在麻醉犬中，吡布特罗和沙丁胺醇的心血管效应相当；它们的效力比异丙肾上腺素弱，作用虽不那么明显，但持续时间更长。
