Positron emission tomography imaging method
Described herein are compositions and methods for diagnosing and/or monitoring pathogenic disease states using positron emission tomography, wherein the pathogenic cells uniquely express, preferentially express, or overexpress vitamin receptors. Also described herein are 18 F conjugates of vitamins and vitamin receptor-binding analogs of the formula.
1. A compound of the formula
wherein V is a folate receptor binding moiety, or an analog thereof; L is an optional bivalent linker; n is an integer selected from 1 to about 5; and Ar is an aryl group, that includes one or more substituents (R f ) m comprising a radiophore or a precursor to a radiophore, where m is an integer selected from 1 to about 3.
2. The compound of claim 1 of the formula
wherein V is a folate receptor binding moiety, or an analog thereof; L is an optional bivalent linker; n is an integer selected from 1 to about 5; R f comprises a radiophore or a precursor to a radiophore; and m is an integer selected from 1 to about 3.
3. The compound of claim 1 wherein the folate receptor binding moiety is folic acid or a folic acid analog.
4. The compound of claim 1 of the formula
wherein L is an optional bivalent linker; n is an integer selected from 1 to about 5; R f comprises a radiophore or a precursor to a radiophore; and m is an integer selected from 1 to about 3.
5. The compound of claim 1 wherein m is 1 or 2.
6. The compound of claim 1 wherein R f comprises one or two nitro groups.
7. The compound of claim 1 wherein R f comprises one or two 18 F fluoro groups.
8. The compound of claim 1 wherein R f comprises at least one nitro group and at least one 18 F fluoro group.
9. The compound of claim 1 wherein the L is a linker comprising a plurality of hydrophilic groups.
10. The compound of claim 9 wherein the plurality of hydrophilic groups are independently selected carbohydrates, or analogs-thereof.
11. The compound of claim 1 wherein L is a linker comprising one or more groups that retard reticuloendothelial system uptake of the conjugate.
12. The compound of claim 1 wherein L is a linker comprising one or more groups that retard liver uptake of the conjugate.
13. A composition comprising a compound of claim 1 , and a carrier therefor, where the compound is present in an amount sufficient for use in positron emission tomography.