Synthesis and activity of partial retro-inverso modified atrial natriuretic factor analogs.

Autor: Berman JM; Merrell Dow Research Institute, Cincinnati, OH., Pelton JT, Hassman CF, Buck SH, Shea PJ, Ertl P, Heminger EF, Broersma RJ
Jazyk: angličtina
Zdroj: International journal of peptide and protein research [Int J Pept Protein Res] 1988 Jul; Vol. 32 (1), pp. 47-55.
DOI: 10.1111/j.1399-3011.1988.tb00925.x
Abstrakt: The synthesis and pharmacological activity of partial retro-inverso modified rat atrial natriuretic factor (rANF) analogs is described. The route to these compounds utilized a combination of solution and solid-phase methods. The analogs prepared all contain a reversed amide bond (psi[NHCO]) at the Ser 25 to Phe26 linkage. This bond has been suggested to play a key role in the metabolic inactivation of ANF. The analogs are of comparable potency to the endogenous peptide rANF1-28 in binding to cultured rat vascular smooth muscle cells, in relaxing serotonin contracted rabbit aortic rings, and as natriuretic/diuretic agents in anesthetized rats. None of the peptides has an extended duration of action in vivo.
Databáze: MEDLINE