Claims
- 1. A reagent for preparing a radiolabeled peptide for imaging sites of intimation within a mammalian body, comprising a specific binding peptide having an amino acid sequence wherein the peptide binds to leukocytes, and a radiolabel-binding moiety selected from the group consisting of moieties of formula
- Cp(aa)Cp
- wherein Cp is a protected cysteine and (aa) is any primary .alpha.- or .beta.-amino acid; and a radiolabel binding moiety comprising a single thiol-containing moiety having the formula
- A--CH(B)--(C(RR')).sub.n --X
- wherein
- A is H, HOOC, H.sub.2 NOC, or --NHOC;
- B is H, SH or NHR", where R" is H, lower alkyl or --C.dbd.O;
- X is SH or NHR", where R" is H, lower alkyl or --C.dbd.O;
- R and R' are independently H or lower alkyl;
- n is 0, 1 or 2;
- and
- where B is NHR", where R" is H, lower alkyl or --C.dbd.O, X is SH and n is 1 or 2;
- where X is NHR", where R" is H, lower alkyl or --C.dbd.O, B is SH and n is 1 or 2;
- where B is H, A is HOOC, H.sub.2 NOC, or --NHOC, X is SH and n is 0 or 1;
- and wherein the thiol moiety is in the reduced form;
- and wherein the radiolabel-binding moiety is covalently linked to the specific binding peptide.
- 2. The reagent of claim 1 wherein the specific binding peptide and the Cp(aa)Cp radiolabel binding moiety are covalently linked through one or more amino acids.
- 3. The reagent of claim 1 wherein the protected cysteine of the Cp(aa)Cp radiolabel binding moiety has a protecting group of the formula
- --CH.sub.2 --NH--CO--R
- wherein R is a lower alkyl having 1 to 6 carbon atoms, 2-,3-,4-pyridyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, carboxy, or lower alkoxycarbonyl.
- 4. The reagent of claim 1 wherein the Cp(aa)Cp radiolabel binding moiety has the formula: ##STR3##
- 5. The reagent of claim 1 wherein the radiolabel is technetium-99m.
- 6. The reagent of claim 1 wherein the specific binding peptide is selected from the group consisting of peptides having the formula:
- pGluGVNDNEEGFFSARC.sub.Acm GC.sub.Acm amide
- (VGVAPG).sub.3 GGGC.sub.Acm GC.sub.Acm amide
- AcC.sub.Acm GC.sub.Acm GGG(VPGVG).sub.4 amide
- AcC.sub.Acm GC.sub.Acm Aca(VPGVG).sub.4 amide,
- and
- (VPGVG).sub.4 GGGC.sub.Acm GC.sub.Acm amide.
- 7. A kit for preparing a radiopharmaceutical preparation, said kit comprising sealed vial containing a predetermined quantity of the reagent of claim 1 and a sufficient amount of reducing agent to label the peptide with technetium-99m.
- 8. A reagent according to claim 1 for preparing a radiolabeled peptide for imaging sites of inflammation within a mammalian body, wherein the reagent comprises a specific binding peptide that is comprised of 4 to 100 amino acids and wherein the peptide binds to leukocytes and is covalently linked to a radiolabel-binding moiety.
- 9. The reagent according to claim 1 wherein the specific binding peptide and the single thiol radiolabel binding moiety are covalently linked through one or more amino acids.
- 10. The reagent according to claim 1 wherein the radiolabel binding moiety is bound to a radiolabel.
- 11. The reagent of claim 10 wherein the radiolabel is Tc-99m.
- 12. A composition of matter comprising the reagent according to claim 8 and a stannous ion.
- 13. A kit for preparing a radiopharmaceutical preparation, said kit comprising sealed vial containing a predetermined quantity of a reagent according to claim 1 and a sufficient mount of reducing agent to label said reagent with Tc-99m.
- 14. The reagent according to claim 1 wherein the peptide is chemically synthesized in vitro.
- 15. The reagent according to claim 14 wherein the peptide is synthesized by solid phase peptide synthesis.
- 16. The reagent according to claim 14 wherein the radiolabel binding moiety is covalently linked to the peptide during in vitro chemical synthesis.
- 17. The peptide according to claim 16 wherein the radiolabel binding moiety is covalently linked to the peptide during solid phase peptide synthesis.
Parent Case Info
This is a divisional of application Ser. No. 08/266,178, filed Jun. 27, 1994, which is a file wrapper continuation of Ser. No. 07/851,074, filed Mar. 13, 1992, now abandoned.
US Referenced Citations (4)
Foreign Referenced Citations (9)
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Non-Patent Literature Citations (1)
Entry |
Moyer et al (1996). J. Nucl. Med, vol. 37, No. 4, pp. 673-679, "Technetium-99m White Blood Cell Specific Imaging Agent Developed from Platelet Factor 4 to Detect Infection." |
Divisions (1)
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Number |
Date |
Country |
Parent |
266178 |
Jun 1994 |
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Continuations (1)
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Number |
Date |
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Parent |
851074 |
Mar 1992 |
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