Ontology highlight
ABSTRACT:
SUBMITTER: Chatterjee J
PROVIDER: S-EPMC4018149 | biostudies-literature | 2011 Jul
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20110404 7
A focused multiply N-methylated library of a cyclic hexapeptidic somatostatin analogue: MK678 cyclo(-MeAYwKVF-) was generated, which resulted in the unexpected observation of an efficacious tetra-N-methylated analogue, cyclo(-MeAYMewMeKVMeF-) with a potent inhibitory action on sensory neuropeptide release in vitro and on acute neurogenic inflammatory response in vivo. The analogue shows selectivity toward somatostatin receptor subtype 2 (sst2). Extensive 2D NMR spectroscopy and molecular dynamic ...[more]