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Design and synthesis of metabolically stable atrial natriuretic factor analogs
Author(s) -
Berman Judd M.,
Chen Teng-Man,
Sargent Roger,
Buck Stephen H.,
Shea Phillip,
Heminger Eileen F.,
Broersma Robert J.
Publication year - 1988
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(88)80175-3
Subject(s) - chemistry , medicine
Two analogs of rat atrial natriuretic factor, rANF 7–28 ‐NH 2 and [Mpr 7 , Ala 2O ,D‐Arg 27 ]rANF 7–27 ‐NH 2 were prepared by the solid‐phase method. These peptides had 2‐fold and 7‐fold less affinity, respectively, than rANF 1–28 in binding to membranes prepared from cultured aortic smooth muscle cells, and both peptides were 5‐fold less potent than rANF 1–28 in relaxing serotonin‐contracted rabbit aortic rings. rANF 7–28 ‐NH 2 was rapidly degraded by rat kidney homogenates but [Mpr 7 Ala 2O ,D‐Arg 27 ]rANF 7–27 ‐NH 2 had enhanced stability against rat kidney homogenate degradation. However, this in vitro stability did not translate into an extended duration of action in vivo.