生长抑素类似物：胰腺腺泡细胞中受体亲和力与环磷酸腺苷生成抑制的相关性

Somatostatin analogs: correlation of receptor affinity with inhibition of cyclic AMP formation in pancreatic acinar cells.

作者信息

Taparel D, Susini C, Esteve J P, Diaz J, Cazaubon C, Vaysse N, Ribet A

出版信息

Peptides. 1985 Jan-Feb;6(1):109-14. doi: 10.1016/0196-9781(85)90085-3.

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.

摘要

生长抑素抑制促胰液素刺激的胰腺腺泡细胞中环磷酸腺苷（cAMP）的生成。这种抑制只是部分性的。最大抑制率约达50%。所测试的生长抑素类似物抑制促胰液素刺激的cAMP生成的效力低于生长抑素。发现半胱氨酸-氮杂丙氨酸-苯丙氨酸-苯丙氨酸-二对氯苯丙氨酸-赖氨酸-苏氨酸-苯丙氨酸-苯丙氨酸-半胱氨酸在抑制促胰液素刺激的cAMP生成方面是生长抑素的拮抗剂。类似物抑制125I-[酪氨酸11]生长抑素与胰腺腺泡的结合。在抑制50%促胰液素刺激的cAMP生成的浓度与受体结合亲和力之间存在良好的相关性（r = 0.97）。