Silbaugh S A, Stengel P W, Rinkema L E
Agents Actions. 1987 Jun;21(1-2):83-8. doi: 10.1007/BF01974926.
The new potent H1 receptor antagonist, LY188695 (KB2413), was delivered to guinea pigs as a pulmonary aerosol and its ability to inhibit histamine-induced airway obstruction examined. Aerosol LY188695 was more effective than inhaled chlorpheniramine or clemastine in reducing the pulmonary gas trapping produced by histamine challenge. Lung antihistamine effects occurred within minutes of a brief, low concentration aerosol exposure and persisted for at least 1 hour. LY188695 aerosol treatment did not produce significant inhibition of methacholine-induced gas trapping. Although systemic antihistamine effects occurred 50 minutes after LY188695 inhalation, aerosol administration produced an enhanced local (i.e., lung) action compared to intravenous delivery.
新型强效H1受体拮抗剂LY188695（KB2413）以肺部气雾剂的形式给予豚鼠，并检测其抑制组胺诱导的气道阻塞的能力。气雾剂LY188695在减轻组胺激发引起的肺气体潴留方面比吸入氯苯那敏或氯马斯汀更有效。在短暂、低浓度气雾剂暴露几分钟内就出现了肺部抗组胺作用，并持续至少1小时。LY188695气雾剂治疗对乙酰甲胆碱诱导的气体潴留没有产生显著抑制作用。虽然在吸入LY188695后50分钟出现了全身抗组胺作用，但与静脉给药相比，气雾剂给药产生了增强的局部（即肺部）作用。
