Dihydroethidine analogues and uses thereof
Tracers for imaging distribution of reactive oxygen species (ROS) are disclosed. The tracers include radiolabeled dihydroethidine (DHE) analogues. Further disclosed are uses of the compounds, including methods of imaging tissue distribution of ROS in vivo by positron emission tomography (PET). Methods of synthesizing the compounds are also disclosed.
1. A radiolabeled compound or salt thereof of structure
wherein R 1 is H or O—R 3 , R 3 is (CH 2 ) q CH 3 ,
q is an integer from 0 to 10; n is an integer from 0 to 3, m is an integer from 0 to 3, p is an integer from 0 to 3, R 2 is methyl or
a is an integer from 0 to 10, wherein at least one atom is a radioisotope and is a bond.
2. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein the radioisotope is a positron-emitting radioisotope.
3. A radiolabeled compound or salt thereof in accordance with claim 1 wherein R 1 is H.
4. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein the compound or salt thereof comprises an 11 CH 3 .
5. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein R 3 is (CH 2 ) q —CH 3 and q is 0.
6. A radiolabeled compound or salt thereof in accordance with claim 5 , wherein R 3 is 11 CH 3 .
7. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein R 3 is
n is an integer from 0 to 3, m is an integer from 0 to 3 and is a bond.
8. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein R 1 is O—R 3 , R 3 is CH 3 .
9. A radiolabeled compound or salt thereof in accordance with claim 8 , wherein R 1 is O—R 3 , wherein R 3 is 11 CH 3 .
10. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein R 1 is O—R 3 , R 3 is
n is an integer from 0 to 3, m is an integer from 0 to 3, F is 18 F and is a bond.
11. A radiolabeled compound or salt thereof in accordance with claim 10 , wherein n is 1.
12. A radiolabeled compound or salt thereof in accordance with claim 10 , wherein m is 2.
13. A radiolabeled compound or salt thereof in accordance with claim 10 , wherein n is 1 and m is 2.
14. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein R 3 is,
p is an integer from 0 to 3, F is 18 F and is a bond.
15. A radiolabeled compound or salt thereof in accordance with claim 13 , wherein p is 2.
16. A radiolabeled compound or salt thereof in accordance with claim 1 , wherein the compound is selected from the group consisting of