title: Somatostatin analogs: correlation of receptor affinity with inhibition of cyclic AMP formation in pancreatic acinar cells.
abstract: 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.
authors.forename: D
authors.initials: D
authors.lastname: Taparel
authors.forename: C
authors.initials: C
authors.lastname: Susini
authors.forename: J P
authors.initials: JP
authors.lastname: Esteve
authors.forename: J
authors.initials: J
authors.lastname: Diaz
authors.forename: C
authors.initials: C
authors.lastname: Cazaubon
authors.forename: N
authors.initials: N
authors.lastname: Vaysse
authors.forename: A
authors.initials: A
authors.lastname: Ribet
mesh_terms: 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
chemical_list: D011956:Receptors, Cell Surface; D017481:Receptors, Somatostatin; D012633:Secretin; D013004:Somatostatin; D000242:Cyclic AMP