| 摘要 |
Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula A-CH2CO-D-Tyr(R)-Phe-Y-Asn-T-U-Z-Q wherein A is 1-adamantyl, cyclohexyl, cyclopentyl, 1-mercaptocyclohexyl, 1-mercaptocyclopentyl, 1-ethyl-1-mercaptopropyl, cyclohexylmethyl, cyclopentylmethyl, methyl, isovaleryl, tert-butyl or phenyl; R is alkyl of 1-4 carbon atoms; Y is Val, Ile, Thr, Ala, Lys, Cha, Nva, Met, Nle, Orn, Ser, Asn, Gln, Phe, Tyr, Gly, Abu or Leu; T is Pen, Abu, Orn, Lys, Arg, Ala, Cha or Thr; U is Pro, Arg, Lys or Orn or a single bond; Z is (D- or L-) Arg, Orn or Lys and Q is Gly(NH2), Arg(NH2), Orn(NH2), Lys(NH2), (D- or L-)Ala(NH2), Ser(NH2), Val(NH2), Phe(NH2), Ile(NH2), The(NH2), Pro(NH2), Tyr(NH2), OH, NHR, NHbzl, NH(CH2)pNH2 or NH(CH2)pOH (wherein R is as above and p is an integer from 2 to 6). Compounds wherein T is Cys have similar activity. |
