P Rekowski, U Galasik-Bartoszek, A Plech, R Brus, G Kupryszewski
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引用次数: 0
摘要
采用固相法合成了[Lys8]-Conopressin G (L1)和[Arg8]-Conopressin S (A1)及其四种类似物。这些类似物是[2-硫代丙酸1,lys8]-抗压素(L2)，[2-硫代丙酸1,Arg8]-抗压素(A2)，[顺-4-甲基-1-硫代环己烷乙酸1,lys8]，抗压素(L3)和[顺-4-甲基-1-硫代环己烷乙酸1,Arg8]-抗压素(A3)。将所有6种多肽与[Arg8]-抗利尿素(AVP)的行为和利尿作用进行比较。抗利尿素A1，和L1及其类似物A2, A3, L2, L3诱导抗利尿作用。注射抗压素后，观察大鼠的转桶行为。
Conopressins and their analogs: synthesis, antidiuretic and behavioral effects.
[Lys8]-Conopressin G (L1), and [Arg8]-Conopressin S (A1) and their four analogs were synthesized using solid phase procedure. These analogs are [2-thiopropionic acid1, lys8]-conopressin (L2), [2-thiopropionic acid1, Arg8]-conopressin (A2), [cis-4-methyl-1-thiocyclohexaneacetic acid1, Lys8], conopressin (L3), and [cis-4-methyl-1-thiocyclohexaneacetic acid1, ARg8]-conopressin (A3). Behavioral and diuretic effects of all six peptides were compared with these of [Arg8]-vasopressin (AVP). Conopressin A1, and L1 and their analogs A2, A3, L2, L3, induced antidiuretic effects. After icv injection of some conopressins, barrel rotatory behavior of rats was observed.
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