Five decapeptides were prepared, each having the generic primary sequence D-Arg0-Arg1-Pro2-Hyp3-Gly4-Thi5-Ser6-X7-Y8-Arg9. A C-terminal β-turn was anticipated when X was an alkyl ether of D-4-hydroxyproline in either the cis or trans geometric state and Y was either a Tic or Oic residue. Whereas cis ethers have only very weak receptor affinities, the trans ethers are signifcantly more potent in binding to guinea pig smooth muscle having K(i) values as low as 0.16 nM. Notably, these peptides do not contain a D-aromatic amino acid at position 7 of the primary sequence.
|Original language||English (US)|
|Number of pages||13|
|Journal||Agents and Actions|
|Issue number||SUPPL. I|
|State||Published - Jan 1 1992|
ASJC Scopus subject areas
- Pharmacology (medical)