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豚鼠反复气雾吸入或肌内注射异丙肾上腺素(简称异丙)5小时,可使该药对抗组胺性哮喘的作用减弱,形成快速耐受性。腹腔注射阿的平或消炎痛,连续3天,有预防作用。反复吸入气雾7天,异丙松弛离体气管的作用减弱。离体气管接触1 μM异丙25分钟,异丙的松弛气管作用、对抗组胺的收缩作用及抑制过敏性收缩作用可产生快速耐受性;阿的平、异搏定、地塞米松和α-萜品烯醇可预防对抗组胺收缩作用的快速耐受性;花生四烯酸可阻断阿的平的预防作用。耐受性主要表现为β受体对激动剂的亲和力降低,其形成与磷脂酶A_2及花生四烯酸有关。
Repeated aerosol inhalation of guinea pigs or intramuscular isoproterenol isoproterenol (referred to as isopropyl) for 5 hours, the drug can reduce the role of antihistamine asthma, the formation of rapid tolerance. A intraperitoneal injection of indomethacin or indomethacin, for 3 consecutive days, have a preventive effect. Repeated inhalation of aerosol for 7 days, isoprene relaxation of the role of isolated trachea weakened. In vitro tracheal exposure to 1 μM isopropyl for 25 minutes, isobaric relaxation of the trachea, against histamine contraction and inhibition of anaphylactic contractions can produce rapid tolerance; A tablet, verapamil, dexamethasone and α Terpineol protects against rapid resistance to histamine contractile effects; arachidonic acid can block the preventive effect of acinar. Tolerance is mainly manifested as a decrease in the affinity of the beta receptor for the agonist, which is associated with phospholipase A2 and arachidonic acid.