Journal article
Synthesis and dopamine receptor modulating activity of unsubstituted and substituted triproline analogues of l-prolyl-l-leucyl-glycinamide (PLG)
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 (RH/RL) of the dopamine receptor, but only 4 was found to increase apomorphine induced rotations in 6-hydroxydopamine-lesioned rats.
Authors
Baures PW; Pradhan A; Ojala WH; Gleason WB; Mishra RK; Johnson RL
Journal
Bioorganic & Medicinal Chemistry Letters, Vol. 9, No. 16, pp. 2349–2352
Publisher
Elsevier
Publication Date
August 1999
DOI
10.1016/s0960-894x(99)00386-8
ISSN
0960-894X