William K. Schmidt

DuP 747: a new, potent, kappa opioid analgesic. Synthesis and pharmacology1.

Abstract The synthesis and pharmacology of (±)-trans-3,4-dichloro-N-methyl-N-[5-methoxy-2-(pyrrolidin-1-yl)-1,2,3,4-tetrahydronaphthalen-1-yl]benzeneacetamide methanesulfonate (DuP 747), a novel kappa agonist analgesic, are described.

DuP 747: sar study☆

Abstract The results of a detailed study of the structure-activity relationships in the series of compounds represented by DuP 747 are described.

Identification of simpler analogs of neurotensin(9–13) which retain antinociceptive activity

Abstract The neurotensin C-terminal pentapeptide has been systematically simplified to identify a minimal fragment with in vivo analgesic activity and neurotensin receptor binding ability. Di-, tri-, and tetrapeptide fragments were inactive. Pentapeptide simplifications established that only the arginine could be replaced with simpler amino acids and retain activity in each assay. The neurotensin C-terminal pentapeptide, Arg-Pro-Tyr-Ile-Leu , is systematically simplified to identify a minimal fragment required for activity in both neurotensin receptor binding and in in vivo analgesic assay.