Patent ID: 6107459
Filing Date: 2000-08-22
Classification: A61K

Abstract:
A reagent comprising a peptide selected from the group consisting ofPLY.Orn.Orn.II.Orn.Orn.LLES (SEQ ID NO.: 26) and QAPLYKKIIKKLLES (SEQ ID NO.: 27), said peptide being covalently linked to a radiolabel-binding moiety selected from the group consisting of:(a)Cp(aa)Cpwherein Cp is a protected cysteine and (aa) is an .alpha.- or .beta.-amino acid;(b) a radiolabel-binding moiety comprising a single thiol having a formulaA--CZ(B)--[C(R.sup.1 R.sup.2)].sub.n --XwhereinA is H, HOOC, H.sub.2 NOC, (peptide)-NHOC, (peptide)-OOC or R.sup.4 ;B is H, SH, --NHR.sup.3, --N(R.sup.3)-(peptide), or R.sup.4 ;X is H, SH, --NHR.sup.3, --N(R.sup.3)-(peptide) or R.sup.4 ;Z is H or R.sup.4 ;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently H or lower straight or branched chain or cyclic alkyl;n is 0, 1 or 2; andwhere B is --NHR.sup.3 or --N(R.sup.3)-(peptide), X is SH, and n is 1 or 2;where X is --NHR.sup.3 or --N(R.sup.3)-(peptide), B is SH, and n is 1 or 2;where B is H or R.sup.4, A is HOOC, H.sub.2 NOC, (peptide)-NHOC, (peptide)-OOC, X is SH, and n is 0 or 1;where A is H or R.sup.4, then where B is SH, X is --NHR.sup.3 or --N(R.sup.3)-(peptide) and where X is SH, B is --NHR.sup.3 or --N(R.sup.3)-(peptide);where X is H or R.sup.4, A is HOOC, H.sub.2 NOC, (peptide)-NHOC, (peptide)-OOC and B is SH;where Z is methyl, X is methyl, A is HOOC, H.sub.2 NOC, (peptide)-NHOC, (peptide)-OOC, B is SH and n is 0; and wherein the thiol moiety is in the reduced form;(c) ##STR5## wherein X=H or a protecting group;(amino acid)=any amino acid;(d) ##STR6## wherein X=H or a protecting group;(amino acid)=any amino acid;(e) ##STR7## wherein each R.sup.5 is independently H, CH.sub.3, or C.sub.2 H.sub.5 ;each (pgp).sup.S is independently a thiol protecting group or H;m, n and p are independently 2 or 3;A=linear or cyclic lower alkyl, aryl, heterocyclyl, a combination thereof or a substituted derivative thereof; and(e) ##STR8## wherein each R.sup.5 is independently H, lower alkyl having 1 to 6 carbon atoms, phenyl, or phenyl substituted with lower alkyl or lower alkoxy;m, n and p are independently 1 or 2;A=linear or cyclic lower alkyl, aryl, heterocyclyl, a combination thereof or a substituted derivative thereof;V=H or --CO-peptide;R.sup.6 =H or peptide;and wherein when V=H, R.sup.6 =peptide and when R.sup.6 =H, V=--CO-peptide.