AP-811, a novel ANP-C receptor selective agonist.
AP-811 is a derivative of the Phe8-Ile15 region of atrial natriuretic peptide (ANP) and is one of the smallest linear ligands for ANP receptors. The binding and agonist activities of AP-811 have been compared with those of other ANP analogs for the ANP-A and ANP-C receptors. AP-811 binds with a high binding affinity to and is a strong agonist for the ANP-C receptor, indicating that the binding and agonist sites for this receptor are the same or near each other in the ANP sequence. In contrast, AP-811 showed no agonistic effect for the ANP-A receptor, although it could bind to this receptor. Comparing the biological activities of AP-811 with those of other ANP analogs, we propose that the binding and agonist sites for the ANP-A receptor may consist of separate regions of ANP. In conclusion, AP-811 is the smallest C-receptor-selective agonist.
Koyama
S
S
New Drug Research Laboratories, Fujisawa Pharmaceutical Co. Ltd., Osaka, Japan.
Inoue
T
T
Terai
T
T
Takimoto
K
K
Kato
M
M
Ito
K
K
Neya
M
M
Seki
J
J
Kobayashi
Y
Y
Kyogoku
Y
Y
D000067956:Adenylyl Cyclase Inhibitors; D000595:Amino Acid Sequence; D009320:Atrial Natriuretic Factor / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D000242:Cyclic AMP / Q000378:metabolism; D006152:Cyclic GMP / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D008024:Ligands; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D017461:Receptors, Atrial Natriuretic Factor / Q000187:drug effects / Q000378:metabolism*
D000067956:Adenylyl Cyclase Inhibitors; D008024:Ligands; D009842:Oligopeptides; C088585:AP 811; D009320:Atrial Natriuretic Factor; D000242:Cyclic AMP; D017461:Receptors, Atrial Natriuretic Factor; D006152:Cyclic GMP