磷酸二酯酶3和4抑制剂降低豚鼠气道高反应性
Reduced airway hyperresponsiveness by phosphodiesterase 3 and 4 inhibitors in guinea-pigs.
作者信息
Germain N, Boichot E, Planquois J M, Lagente V
机构信息
INSERM U456, Laboratoire de Pharmacodynamie et de Pharmacologie Moléculaire, Faculté des Sciences Pharmaceutiques et Biologiques, Université de Rennes 1, France.
出版信息
Mediators Inflamm. 1999;8(3):153-7. doi: 10.1080/09629359990487.
The aim of the present study was to compare the effects of selective phosphodiesterase (PDE) 3, 4 and 5 inhibitors on antigen-induced airway hyperresponsiveness in sensitized guinea-pigs. When the sensitized guinea-pigs were orally pre-treated with the selective PDE4 inhibitor, Ro 20-1724 (30 mg/kg), and studied 48h after OA, a significant reduction (P<0.01) of the leftward shift of the dose-response curve to ACh was noted, whereas it was ineffective at the lower dose (10 mg/kg). Administration of the selective PDE3 inhibitor, milrinone (30 mg/kg) also elicited a significant reduction (P<0.01) of the airway hyperresponsiveness, whereas the PDE5 inhibitor zaprinast (30 mg/kg) was ineffective. These results show that both PDE3 and PDE4 inhibitors are able to inhibit the antigen-induced airway hyperresponsiveness in sensitized guinea-pigs and support the potential utility of selective PDE inhibitors in the treatment of asthma.
本研究的目的是比较选择性磷酸二酯酶（PDE）3、4和5抑制剂对致敏豚鼠抗原诱导的气道高反应性的影响。当致敏豚鼠口服选择性PDE4抑制剂Ro 20-1724（30 mg/kg）并在卵清蛋白激发后48小时进行研究时，发现乙酰胆碱剂量反应曲线向左移位显著降低（P<0.01），而在较低剂量（10 mg/kg）时无效。给予选择性PDE3抑制剂米力农（30 mg/kg）也可显著降低（P<0.01）气道高反应性，而PDE5抑制剂扎普司特（30 mg/kg）则无效。这些结果表明，PDE3和PDE4抑制剂均能够抑制致敏豚鼠抗原诱导的气道高反应性，并支持选择性PDE抑制剂在哮喘治疗中的潜在应用价值。
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