Compounds acting as antagonists of the antidiuretic/and or vasopressor activity of arginine vasopressin are those of the formula A--CH2 CO--D--Tyr(R)--Phe--Y--Asn--T--U--Z--Qwherein A is a-adamantyl, cyclohexyl, cyclopentyl, 1-mercaptocyclohexyl, 1-mercaptocyclopentyl, 1-ethyl-1-mercaptopropyl, yclohexylmethyl, cyclopentylmethyl, methyl, isopropyl, 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, Oys, 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), Thr(NH2), Pro(NH2), Tyr(NH2), NH2, OH, NHR, NGbzl, NH(CH2)p NH2 or NH(CH2)p OH, wherein R is as above and p is an integer from 2 to 6. Compounds wherein T is Cys have similar activity.

Document Type


Primary Class


Secondary Class

514/15.4; 514/807; 530/315; 530/317; 530/328; 530/329

Application Number


Filing Date

June 1987

Patent Number



Medical College of Ohio; The Trustees of Columbia University

Publication Date


Patent Country





The University of Toledo


University of Toledo Libraries

Digital Publisher

Digital Initiatives


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Rights Statement

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