Somatostatin analogs: correlation of receptor affinity with inhibition of cyclic AMP formation in pancreatic acinar cells.
Somatostatin inhibited secretin-stimulated cyclic AMP formation in pancreatic acinar cells. The inhibition was only partial. Maximal inhibition reached about 50%. Somatostatin analogs tested inhibited secretin-stimulated cyclic AMP formation with a lower potency than somatostatin. Cys-Aza Ala-Phe-Phe-DTrp-Lys-Thr-Phe-Phe-Cys was found to be an antagonist of somatostatin in inhibiting secretin-stimulated cyclic AMP. Analogs inhibited the binding of 125I-[Tyr11] somatostatin to pancreatic acini. There was a good correlation (r = 0.97) between concentration for inhibiting 50% secretin-stimulated cyclic AMP and receptor binding affinities.
Taparel
D
D
Susini
C
C
Esteve
J P
JP
Diaz
J
J
Cazaubon
C
C
Vaysse
N
N
Ribet
A
A
D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D000242:Cyclic AMP / Q000378:metabolism; D006168:Guinea Pigs; D007700:Kinetics; D010179:Pancreas / Q000378:metabolism*; D011956:Receptors, Cell Surface / Q000378:metabolism*; D017481:Receptors, Somatostatin; D012633:Secretin / Q000037:antagonists & inhibitors*; D013004:Somatostatin / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship
D011956:Receptors, Cell Surface; D017481:Receptors, Somatostatin; D012633:Secretin; D013004:Somatostatin; D000242:Cyclic AMP