Claims
- 1. A complex formed by reacting a reagent comprising a leukocyte-binding chemotactic peptide covalently linked to a radiolabel-binding moiety selected from the group consisting of:
- Cp(aa)Cp
- wherein Cp is a protected cysteine and (aa) is any primary .alpha.- or .beta.-amino acid;
- a radiolabel-binding moiety comprising a single thiol-containing moiety having a 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", X is SH and n is 1 or 2;
- where X is NHR", B is SH and n is 1 or 2;
- where B is H, X is SH and n is 0 or 1;
- and wherein the thiol moiety is in the reduced form;
- and a radiolabel-binding moiety of formula ##STR3## wherein each R is independently H, lower alkyl having one to six carbon atoms, phenyl, or phenyl substituted with lower alkyl or lower alkoxy, and wherein each n is independently one or 2,
- with technetium-99m in the presence of a reducing agent, wherein the complex is capable of accumulating at a site of inflammation in a mammalian body.
- 2. The complex of claim 1, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion, a solid-phase reducing agent, and a ferrous ion.
- 3. The complex of claim 1, formed by ligand exchange of a prereduced technetium-99m complex.
- 4. A method for preparing an imaging agent for detecting infection or inflammation in a mammalian body comprising the steps of
- a) providing a reagent comprising a leukocyte-binding chemotactic peptide covalently linked to a radiolabel-binding moiety selected from the group consisting of
- Cp(aa)Cp
- wherein Cp is a protected cysteine and (aa) is any primary .alpha.- or .beta.-amino acid;
- a radiolabel-binding moiety comprising a single thiol-containing moiety having a 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", X is SH and n is 1 or 2;
- where X is NHR", B is SH and n is 1 or 2;
- where B is H, X is SH and n is 0 or 1;
- and wherein the thiol moiety is in the reduced form;
- and a radiolabel-binding moiety of formula ##STR4## wherein each R is independently H, lower alkyl having one to six carbon atoms, phenyl, or phenyl substituted with lower alkyl or lower alkoxy, and wherein each n is independently one or 2, and
- b) reacting the reagent with technetium-99m in the presence of a reducing agent.
- 5. The method of claim 4, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion, a ferrous ion, and a solid-phase reducing agent.
- 6. A method for preparing an imaging agent for detecting infection or inflammation in a mammalian body comprising the steps of
- a) providing a reagent comprising a leukocyte-binding chemotactic peptide covalently linked to a radiolabel-binding moiety selected from the group consisting of
- Cp(aa)Cp
- wherein Cp is a protected cysteine and (aa) is any primary .alpha.- or .beta.-amino acid;
- a radiolabel-binding moiety comprising a single thiol-containing moiety having a 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", X is SH and n is 1 or 2;
- where X is NHR", B is SH and n is 1 or 2;
- where B is H, X is SH and n is 0 or 1;
- and wherein the thiol moiety is in the reduced form;
- and a radiolabel-binding moiety of formula ##STR5## wherein each R is independently H, lower alkyl having one to six carbon atoms, phenyl, or phenyl substituted with lower alkyl or lower alkoxy, and wherein each n is independently one or 2, and
- b) labeling the reagent with technetium-99m by ligand exchange of a prereduced technetium-99m complex.
- 7. A complex formed by reacting technetium-99m with a reagent comprising a leukocyte-binding chemotactic peptide covalently linked to a radiolabel-binding moiety, wherein the technetium-99m complexed radiolabel-binding moiety has a net charge of -1, and wherein the complex is capable of accumulating at a site of inflammation in a mammalian body.
- 8. The complex of claim 7, formed by reacting the reagent with technetium-99m in the presence of a reducing agent.
- 9. The complex of claim 8, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion, a solid-phase reducing agent, and a ferrous ion.
- 10. The complex of claim 7 formed by reacting the reagent with technetium-99m by ligand exchange of a prereduced technetium-99m complex.
- 11. A method for preparing an imaging agent for detecting infection or inflammation in a mammalian body comprising the steps of
- a) providing a reagent comprising a leukocyte-binding chemotactic peptide covalently linked to a radiolabel-binding moiety capable of forming a complex with technetium-99m having a net charge of -1; and
- b) labeling the reagent with technetium-99m by ligand exchange of a prereduced technetium-99m complex.
- 12. A complex formed by reacting technetium-99m with a reagent comprising a chemotactic peptide which binds to leukocytes covalently linked to a radiolabel-binding moiety, wherein the technetium-99m and the radiolabel-binding moiety form a neutral complex, and wherein the complex is capable of accumulating at a site of inflammation in a mammalian body.
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 (7)
Divisions (1)
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Number |
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266178 |
Jun 1994 |
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Continuations (1)
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851074 |
Mar 1992 |
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