Galanin is a neuropeptide initiating its multiple biological effects by bin
ding to different subtypes of seven transmembrane spanning galanin receptor
s, thus transducing the extracellular signal to G-proteins. There is a wide
range of galanin receptor ligands available today, and some of the ligands
have been shown to act as antagonists in galaninergic signal transduction
systems at tissue level and in vivo. Subtype-specific galanin receptor liga
nds could be used selectively to initiate or block the effects of galanin i
n order to provide insights into the role of galanin both at normal and pat
hophysiological conditions, and in the development of compounds with therap
eutical values. This review highlights the recent reports on the binding af
finities of GalR in CNS and transfected cell lines. (C) 2000 Harcourt Publi
shers Ltd.