Marthan R
Laboratoire de Physiologie Cellulaire Respiratoire, Faculté de Médecine Victor-Pachon, Université Victor-Segalen, Bordeaux.
Rev Mal Respir. 1998 Jun;15(3):219-24.
The understanding of cellular and molecular mechanisms involved in the contraction of airway smooth muscle has tremendously advanced in the recent years. Among extracellular messengers that control airway smooth muscle contraction attention has focused on leukotrienes since several strategies for pharmacological interventions in either the production or the effect of these substances have been developed. Two types of receptor, CysLT and BLT, coupled to G proteins, have been identified and airway smooth muscle contraction mostly depends on CysLT1 receptor activation. This activation induces intracellular calcium release leading to an increase in cytoplasmic calcium concentration responsible for airway smooth muscle contraction. Leukotriene antagonists are now available and their role in asthma treatment is being defined.
近年来,对气道平滑肌收缩所涉及的细胞和分子机制的理解有了极大的进展。在控制气道平滑肌收缩的细胞外信使中,白三烯受到了关注,因为已经开发出了几种针对这些物质的产生或作用进行药物干预的策略。已经鉴定出两种与G蛋白偶联的受体,即半胱氨酰白三烯受体(CysLT)和白三烯B4受体(BLT),气道平滑肌收缩主要依赖于CysLT1受体的激活。这种激活诱导细胞内钙释放,导致细胞质钙浓度升高,从而引起气道平滑肌收缩。白三烯拮抗剂现已可用,它们在哮喘治疗中的作用正在得到明确。