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Synthesis, antidiuretic and pressor activities of [arginine4]arginine-vasopressin and two related analogues.

作者信息

Rekowski P, Lammek B, Melin P, Ragnarsson U, Kupryszewski G

出版信息

Acta Chem Scand B. 1985;39(6):453-7. doi: 10.3891/acta.chem.scand.39b-0453.

DOI:10.3891/acta.chem.scand.39b-0453
PMID:4060959
Abstract

Using well-established solid-phase techniques, three new analogues of arginine-vasopressin (AVP) were synthesized. In these the glutamine residue in position 4 was replaced with an additional arginine. The new analogues were: [Arginine4]arginine-vasopressin ([Arg4]AVP), [2-thiopropionic acid1,arginine4]arginine-vasopressin (d[Arg4]AVP) and [1-thiocyclohexaneacetic acid1,arginine4]arginine-vasopressin (d(CH2)5[Arg4]AVP). [Arg4]AVP showed about the same antidiuretic activity as AVP but had only about 40% of its pressor activity. Unexpectedly, deamination caused a drop in the antidiuretic activity to about 50%. d(CH2)5[Arg4]AVP had practically negligible antidiuretic and low pressor effects.

摘要

相似文献

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引用本文的文献

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Synthesis of three NH2-terminally extended arginine-vasopressins with prolonged biological activities.
Experientia. 1987 Dec 1;43(11-12):1211-2. doi: 10.1007/BF01945528.
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Invertebrate neuropeptides resembling vasotocin and some analogues: synthesis and pharmacological properties.类似于血管紧张素及其某些类似物的无脊椎动物神经肽：合成与药理学特性。
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