Lu Xiaoying, Lundström Linda, Langel Ulo, Bartfai Tamas
Department of Neuropharmacology, The Harold L. Dorris Neurological Research Center, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Neuropeptides. 2005 Jun;39(3):143-6. doi: 10.1016/j.npep.2004.12.012. Epub 2005 Feb 1.
The three galanin receptor subtypes (GalR1-3) belong to the G protein-coupled receptor superfamily. The widespread distribution of galanin and its receptors in the CNS and PNS and the numerous physiological and pharmacological effects of galanin (for review, cf. Vrontakis, 2002) render the three galanin receptors attractive drug targets. The industrial efforts, however, have not yet resulted in a wealth of receptor subtype specific agonists or antagonists with high affinity and selectivity. The present paper summarizes the properties of the galanin ligands used at the end of 2004 in the ca. 2000 publications and complements their pharmacological characterization with new data.
三种甘丙肽受体亚型（GalR1 - 3）属于G蛋白偶联受体超家族。甘丙肽及其受体在中枢神经系统和外周神经系统中广泛分布，且甘丙肽具有众多生理和药理作用（综述见Vrontakis，2002），这使得三种甘丙肽受体成为颇具吸引力的药物靶点。然而，业界的努力尚未产生大量具有高亲和力和选择性的受体亚型特异性激动剂或拮抗剂。本文总结了截至2004年底约2000篇出版物中所使用的甘丙肽配体的特性，并用新数据补充了它们的药理学特征。
