de Tullio P, Delarge J, Pirotte B
Department of Medicinal Chemistry, Université de Liège, CHU, Avenue de l'Hôpital 1, B-4000 Sart-Tilman (Liège), Belgium.
Expert Opin Investig Drugs. 2000 Jan;9(1):129-46. doi: 10.1517/13543784.9.1.129.
Cholecystokinin (CCK) is an important 'brain-gut' hormone located both in the gastrointestinal (GI) system and in the CNS. At least two different G-coupled high affinity receptors have been identified: the CCK-A and the CCK-B receptors. Although the complex biological role of CCK is, as yet, not fully understood, its connection with many different physiological processes both at the GI level and at the CNS level is now well established. There is much potential for therapeutic use of CCK receptor ligands, however, clear investigations have yet to be completed. Several chemical families have been investigated over the last 20 years to find potent, subtype selective and stable CCK receptor agonists and antagonists. The main goal was to discover new therapeutic drugs acting on GI and/or on CNS diseases and also, to obtain powerful pharmacological tools that could permit a better understanding of the biological role of CCK. Despite promising results from investigations into medicinal chemistry of CCK receptor ligands, the therapeutical applications of these ligands still remains to be defined. This article reviews the main biological role of CCK, the therapeutic potential of CCK-A and CCK-B receptor agonists and antagonists and the common compounds from the different families of ligands.
胆囊收缩素（CCK）是一种重要的“脑-肠”激素，存在于胃肠道（GI）系统和中枢神经系统（CNS）中。现已鉴定出至少两种不同的G蛋白偶联高亲和力受体：CCK-A受体和CCK-B受体。尽管CCK复杂的生物学作用尚未完全明确，但目前已充分证实其与胃肠道水平和中枢神经系统水平的许多不同生理过程相关。CCK受体配体具有很大的治疗应用潜力，然而，明确的研究尚未完成。在过去20年中，已对多个化学家族进行了研究，以寻找强效、亚型选择性和稳定的CCK受体激动剂和拮抗剂。主要目标是发现作用于胃肠道和/或中枢神经系统疾病的新型治疗药物，同时获得强大的药理学工具，以便更好地理解CCK的生物学作用。尽管CCK受体配体的药物化学研究取得了一些有前景的结果，但这些配体的治疗应用仍有待确定。本文综述了CCK的主要生物学作用、CCK-A和CCK-B受体激动剂及拮抗剂的治疗潜力，以及不同配体家族的常见化合物。
