Synthesis and dopamine receptor modulating activity of unsubstituted and substituted triproline analogues of L-prolyl-L-leucyl-glycinamide (PLG)

Paul W. Baures, Ashish Pradhan, William H. Ojala, William B. Gleason, Ram K. Mishra, Rodney L. Johnson

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

Triprolines Pro-Pro-Pro-NH2 (4), Pro-Pro-D-Pro-NH2 (5), Pro-Pro(trans- 3-Me)-D-Pro-NH2 (6), and Pro-Pro(cis-3-Me)-D-Pro-NH2 (7) were made as conformationally constrained analogues of Pro-Leu-Gly-NH2. Triprolines 4-6 produced significant increases in the high- and low-affinity state ratio (R(H)/R(L)) of the dopamine receptor, but only 4 was found to increase apomorphine induced rotations in 6-hydroxydopamine-lesioned rats.

Original languageEnglish (US)
Pages (from-to)2349-2352
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume9
Issue number16
DOIs
StatePublished - Aug 16 1999

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