Reduced amide bond neurotensin 8-13 mimetics with potent in vivo activity

Abstract Appropriately substituted 8–9 (ΨCH 2 NH) isosteres of neurotensin (NT) 8–13 have been found which are active as NT agonists in vitro and in vivo . SAR studies suggest that preventing amide bond hydrolysis at the 8–9 and 11–12 positions of NT(8–13) mimetics is important for producing compounds with potent activity in vivo . Other simplified replacements for the Arg-Arg portion of NT(8–13) are reported.