Conformational analysis and mu-opioid receptor affinity of short peptides, endomorphin models in a low polarity solvent.
Peptide carbamates containing the sequence H-Pro-Trp-PheNH2 showed in CDCl3 restricted conformations stabilized by the presence of a gamma-turn. To test the reliability of the peptides as endomorphin conformational models, we measured the affinities for mu-receptors labelled with [3H]-DAMGO. In particular, Cbz-Pro-Trp-PheNH2 displayed a nanomolar affinity.
D000818:Animals; D002219:Carbamates / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011487:Protein Conformation; D051381:Rats; D017450:Receptors, Opioid, mu / Q000187:drug effects*; D012997:Solvents / Q000737:chemistry; D013055:Spectrophotometry, Infrared; D013696:Temperature
D002219:Carbamates; D008024:Ligands; D009842:Oligopeptides; D017450:Receptors, Opioid, mu; D012997:Solvents; C105293:endomorphin 1