L-dopa potentiating analogs of Pro-Leu-Gly-NH2 with oral efficacy.
Chemical modification of PLG, comprising replacement of proline or/and leucine by unnatural amino acids led to analogs with high oral efficacy. The most active analog identified in the course of our works was 1-prolyl-2-phenyl-1-2-aminobutanoylglycinamide (Doreptide). Doreptide is presently further evaluated as a new drug for the treatment of Parkinson's disease.
BASF, Hauptlaboratorium, Ludwigshafen, F.R.G.
H P
HP
Albrecht
H P
HP
Hofman
G
G
Klebe
H
H
Kreiskott
D000284:Administration, Oral; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D004357:Drug Synergism; D007980:Levodopa / Q000494:pharmacology*; D009075:MSH Release-Inhibiting Hormone / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000494:pharmacology*; D008297:Male; D051379:Mice
D007980:Levodopa; D009075:MSH Release-Inhibiting Hormone