CONSTRAINED ANALOGS OF THE CALCITONIN-GENE-RELATED PEPTIDE

The calcitonin gene-related peptide, CGRP, has potential medicinal use for instance as a vasodilator or in the regulation of bone metabolism . In this study new analogues of CGRP based on molecular modelling of active fragments were synthesised and tested. The analogues were found to have affinities for the receptor comparable to those seen for nati ve CGRP. Two analogues were found to be agonists. The analogues give a n insight to the bioactive conformation of CGRP as they were constrain ed by disulphide, bridges. (C) 1994 Academic Press, Inc.