Contulakin-G, analogs thereof and uses therefor

A method for treating pain in an individual which comprises administering an analgesic effective amount of an active agent to an individual in need of pain treatment, said active agent is selected from the group consisting of

• (a) a generic contulakin-G having the following general formula Xaa1-Xaa2-Xaa3-Xaa3-Gly-Gly-Xaa2-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Ile-Leu (SEQ ID NO:2), where Xaa1 is pyro-Glu, Glu, Gln or γ-carboxy-Glu;
• Xaa2 is Ser, Thr or S-glycan modified Cys;
• Xaa3 is Glu or γ-carboxy-Glu;
• Xaa4 is Asn, N-glycan modified Asn or S-glycan modified Cys;
• Xaa5 is Ala or Gly;
• Xaa6 is Thr, Ser, S-glycan modified Cys, Tyr or any hydroxy containing unnatural amino acid;
• Xaa7 is Lys, N-methyl-Lys, N,N-dimethyl-Lys, N,N,N-trimethyl-Lys, Arg, ornithine, homoarginine or any unnatural basic amino acid;
• Xaa8 is Ala, Gly, Lys, N-methyl-Lys, N,N-dimethyl-Lys, N,N,N-trimethyl-Lys, Arg, ornithine, homoarginine, any unnatural basic amino acid or X-Lys where X is (CH2)n, phenyl, —(CH2)m—(CH═CH)—(CH2)mH or —(CH2)m—(C≡C)—(CH2)mH in which n is 1-4 and m is 0-2;
• Xaa9 is Pro or hydroxy-Pro;
• and Xaa10 is Tyr, mono-iodo-Tyr, di-iodo-Tyr, O-sulpho-Tyr, O-phospho-Tyr, nitro-Tyr, Trp, D-Trp, bromo-Trp, bromo-D-Trp, chloro-Trp, chloro-D-Trp, Phe, L-neo-Trp, or any unnatural aromatic amino acid, with the proviso that the generic contulakin-G is not un-glycosylated contulakin-G;
• (b) a generic contulakin-G of (a) which is modified to contain an O-glycan, an S-glycan or an N-glycan;
• (c) a contulakin-G analog which comprises an N-terminal truncation of from 1 to 9 amino acids of the generic contulakin-G of (a);
• (d) a contulakin-G analog of (c), wherein a Ser-O-glycan, Thr-O-glycan or Cys-S-glycan is substituted for the amino acid residue at the truncated N-terminus;
• (e) a contulakin-G analog, wherein a Ser-O-glycan, Thr-O-glycan or Cys-S-glycan is substituted for a residue at positions 1-9 of the generic contulakin-G of (a);
• and
• (f) a contulakin-G analog which comprises an N-terminal truncation of 10 amino acids of the generic contulakin-G of (a) which is further modified to contain a Lys-N-glycan at residue 11 of the generic contulakin-G.