Related Experiment Videos
Synthesis of enkephalin analogs. Part V. N-monosubstituted derivatives
R Paruszewski1, R Matusiak, G Rostafińska-Suchar
1Department of Pharmaceutical Chemistry, Medical Academy, Warszawa, Poland.
Polish Journal of Pharmacology and Pharmacy
|March 1, 1991
Abstract:
Synthesis of four new derivatives of enkephalin analogs: H-BuTyr-DMet-Gly- Phe-epsilon Ahx-OH 9, H-BzlTyr-DMet-Gly-Phe-epsilon Ahx-OH 12, H-Butyr-DMet-Gly- -Phe-epsilon Ahx-epsilon Ahx-OH 15 and H-BzlTyr-DMet-Gly-Phe-epsilon Ahx-OH is reported. They were examined for agonistic, antagonistic and analgesic activity. Compound 12 is the most potent among investigated peptides. Its agonistic activity in vitro is 7.85 x 10(-8) M/l (GPI) and 9.5 x 10(-7) M/l (MVD). None of the peptides showed antagonistic activity. Only compound 12 showed weak, not dose-dependent analgesic activity in rats.