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皮下注射生长抑素类似物是延长作用时间的主要因素。

Subcutaneous administration of somatostatin analogs as a major factor in the enhancement of the duration of action.

作者信息

Torchiana M L, Cook P G, Wiese S R, Saperstein R, Veber D F

出版信息

Arch Int Pharmacodyn Ther. 1978 Sep;235(1):170-6.

PMID:736688
Abstract

Somatostatin and Des(Ala1Gly2)desaminol[Cys3]descarboxy-]Cys14[-]D-Trp8[dicarba3,14-somatostatin (Ia) are more potent inhibitors of glucagon, insulin and growth hormone release than the L-Trp8 analog (Ib). However when infused intravenously, these three compounds are equipotent but short-acting inhibitors of pentagastrin evoked gastric secretion in the dog. The duration of inhibition of equieffective antisecretory doses is significantly increased following subcutaneous administration 30 min prior to a food stimulus. The longest duration of antisecretory action is seen with the D-Trp8 analog (Ia) after subcutaneous administration.

摘要

生长抑素和去(丙氨酸1甘氨酸2)脱氨基-[半胱氨酸3]脱羧基-[半胱氨酸14]-D-色氨酸8[二碳3,14-生长抑素(Ia)比L-色氨酸8类似物(Ib)更有效地抑制胰高血糖素、胰岛素和生长激素的释放。然而,当静脉注射时,这三种化合物在抑制狗的五肽胃泌素诱发的胃液分泌方面效力相当但作用时间短。在食物刺激前30分钟皮下给药后,等效抗分泌剂量的抑制持续时间显著延长。皮下给药后,D-色氨酸8类似物(Ia)的抗分泌作用持续时间最长。

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