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NOVEL ANTAGONISTS OF THE ANTIDIURETIC AND OR VASOPRESSOR ACTION OF ARGININE VASOPRESSION
NOVEL ANTAGONISTS OF THE ANTIDIURETIC AND OR VASOPRESSOR ACTION OF ARGININE VASOPRESSION
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机译：精氨酸血管加压药的抗血管紧张药和/或血管加压药作用的新型拮抗剂
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摘要
Vasopressin analogs (I)(X1=CH3, C2H5,n-Pro, iso-Pro or butyl; Tyr is L- or D-; W is Pro of delta3-Pro; Z=L-or D-Arg) were prepd. and used for antagonising antidiuretic and vesopressor action of arginine vasopressin. Thus, Boc-Tyr(Me)-Phe-Gln-Asn-Cys(CH2Ph)Pro-Arg(Tos)- Gly-NH2(Boc=Me3CO2C, Tos=tosyl), prepd. by the solidphase method, was deblocked by CF3CO2H and then condensed with cyclohexaneacetate deriv. (II) to give peptide amide (III). (III) was deblocked by Na/ NH3 and then cyclized by oxidn. to give (I) (X1=G1n, W=Pro, Z=Arg).
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机译：制备了加压素类似物（I）（X 1 ＝ CH 3，C 2 H 5，n-Pro，iso-Pro或丁基; Tyr是L-或D-; W是delta3-Pro的Pro; Z ＝ L-或D-Arg）。并用于拮抗精氨酸加压素的抗利尿剂和升压药作用。因此，制备Boc-Tyr（Me）-Phe-Gln-Asn-Cys（CH 2 Ph）Pro-Arg（Tos）-Gly-NH 2（Boc ＝ Me 3 CO 2 C，Tos ＝甲苯磺酰基），制备。通过固相法，用CF 3 CO 2 H解封，然后与环己烷乙酸酯缩合。 （II）得到肽酰胺（III）。 （III）用Na / NH3脱保护，然后通过氧化环化。给出（I）（X1 = G1n，W = Pro，Z = Arg）。
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