Abstract
Appropriately substituted 8–9 (ΨCH 2NH) 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.
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