Radiolabeled compounds for in vivo imaging of gastrin-releasing peptide receptor (grpr) and treatment of grpr-related disorders

A peptidic compound, wherein the compound has the structure of Formula A or is a salt or solvate of Formula A,

• (A)
• Rradn6-[linker]-RL-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-
• Xaa7-Xaa8-ψ-Xaa9-NH2
• wherein:
• Xaa1 is an N-terminal amino acid residue selected from D-Phe, 4-chlorophenylalanine (Cpa), D-Cpa, 3-(1-naphthyl)alanine (Nal), D-Tpi, D-Nal, 3-(2-naphthyl)alanine (2-Nal), or D-2-Nal;
• Xaa2 is Asn, Gln, homoserine (Hse), citrulline (Cit) or His;
• Xaa3 is Trp, β-(3-benzothienyl)alanine (Bta), or Tpi;
• Xaa4 is Ala or Ser;
• Xaa5 is Val or tert-leucine (Tle);
• Xaa6 is Gly, NMe-Gly, or D-Ala;
• Xaa7 is His or NMe-His;
• Xaa8 is Leu, D-Pro, or Phe;
• Xaa9-NH2 is a C-terminally amidated amino acid residue selected from Pro or thiazoline-4-carboxylic acid (Thz);
• ψ represents a peptide bond or reduced peptide bond joining Xaa8 to Xaa9;
• -[linker]-RL— is a 4-amino-(1-carboxymethyl)piperidine (Pip) linker, a 9-amino-4,7-dioxanonanoic acid (dPEG2) linker, or a 4-(2-aminoethyl)-1-carboxymethyl-piperazine (Acp) linker;
• an albumin binder (Ralb) is optionally bonded to an L1 of the linker, wherein the albumin binder is:
• —(CH2)n3—CH3 wherein n3 is 8-20;
• —(CH2)n4—C(O)OH wherein n4 is 8-20;
• wherein n5 is 1-4 and R3a is H or methyl, and R3b is I, Br, F, Cl, H, OH, OCH3, NH2, NO2 or C1-C6 alkyl;
• or
• n6 is 1-5;
• and
• each Rrad is a radiolabeling group bonded to the linker, wherein the radiolabeling group is a radiometal chelator.