1. Chu, M.; Mierzwa, R.; Truummes, I.; King, A.; Sapidou, E.; Barrabee, E.; Terracciano, J.; Patel, M. G.; Gullo, V. P.; Burrier, R.; Das, P. R.; Mittelmann, S.; Paur, M. S. Tetrahedron Lett. 1997, 38, 6111–6114.
2. It is noteworthy that Sch 202596 (1) is the only small molecule to date shown to inhibit [125I]-galanin binding to GalR1-containing membranes prepared from human melanoma cells using a radioligand competition assay (IC50=1.7 μM).1
3. So far, three galanin receptor subtypes, GalR1, GalR2, and GalR3, have been cloned and characterized. For a recent review on the galanin receptors as novel therapeutic targets, see: Wang, S.; Gustafson, E. L. Drug News Perspect. 1998, 11, 458–468.
4. (a) Crawley, J. N.; Robinson, J. K.; Langel, Ü.; Bartfai, T. Brain Res. 1993, 600, 268–272.
5. (b) Rowland, N. E.; Kalra, S. P. CNS Drugs 1997, 419–426.