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Details for Patent: 5,750,089

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Details for Patent: 5,750,089

Title: Halogenated neuroprobe for mapping monoamine reuptake sites
Abstract:An iodinated neuroprobe is provided for mapping monoamine reuptake sites. The iodinated neuroprobe is of the formula: ##STR1## wherein R= ##STR2## wherein n=2-8; R'=C.sub.w H.sub.2w+1 wherein w=0-6 and C includes an isotope of carbon; and X=an isotope of Cl, an isotope of Br, an isotope of F, an isotope of I, or Sn(R".sub.1 R".sub.2 R".sub.3), wherein R".sub.1 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group; R".sub.2 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group; and R".sub.3 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group. Additionally, a precursor of a radiolabeled neuroprobe and a kit for preparing the iodinated neuroprobe are provided.
Inventor(s): Neumeyer; John L. (Wayland, MA), Milius; Richard A. (Boston, MA), Tamagnan; Gilles (Framingham, MA), Wang; Shaoyin (Lexington, MA)
Assignee: Neuro Imaging Technologies, LLC (Boston, MA)
Filing Date:Jan 11, 1996
Application Number:08/584,617
Claims:1. A neuroprobe having the formula: ##STR5## wherein R= ##STR6## wherein n=2-8; R'=C.sub.w H.sub.2w+1 wherein w=0-6 and C includes an isotope of carbon; and

X=an isotope of Cl, an isotope of Br, an isotope of F, an isotope of I, or Sn(R".sub.1 R".sub.2 R".sub.3), wherein

R".sub.1 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group;

R".sub.2 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group; and

R".sub.3 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group.

2. The neuroprobe of claim 1, wherein said isotope of I is .sup.123 I.

3. The neuroprobe of claim 1, wherein said isotope of I is .sup.125 I.

4. The neuroprobe of claim 1, wherein said isotope of I is .sup.131 I.

5. The radiolabeled neuroprobe of claim 1, wherein in R', C includes a radioactive isotope of carbon.

6. A kit for preparing a radiolabeled neuroprobe for mapping monoamine reuptake sites, the kit comprising: a precursor of the formula: ##STR7## wherein R= ##STR8## wherein n=2-8; R'=C.sub.w H.sub.2w+1 wherein w=0-6 and C includes an isotope of carbon; and

X=a non-radioactive isotope of Cl, a nonradioactive isotope of Br, a non-radioactive isotope of F, a non-radioactive isotope of I, or Sn(R".sub.1 R".sub.2 R".sub.3), wherein

R".sub.1 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group;

R".sub.2 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group; and

R".sub.3 =a C.sub.p H.sub.2p+1 group where p=1-6, or an aryl group.

7. The kit of claim 6, wherein the precursor is reacted in the presence of a radioisotope source.

8. The kit of claim 7, wherein the radioisotope source is a solution of a salt of a radioactive isotope of iodine, and the reaction takes place in the presence of an oxidizing agent.

9. The kit of claim 8, wherein said radioactive isotope of iodine is .sup.123 I.

10. The kit of claim 8, wherein said radioactive isotope of iodine is .sup.125 I.

11. The kit of claim 8, wherein said radioactive isotope of iodine .sup.131 I.

12. The kit of claim 7, wherein said radioisotope source is .sup.18 F.

13. The kit of claim 12, wherein the radioisotope source is selected from the group consisting of Na.sup.18 F, K.sup.18 F, and Cs.sup.18 F.

14. The kit of claim 12, wherein said .sup.18 F is complexed with a reagent of the formula M.sup.+ X.sup.-, wherein:

M.sup.+ =a complex of 4,7,13,16,21,24-hexaoxa-1,10-diazabicyclo-[8.8.8]hexacosane and one of K, Na, Ce, Ru, a tetraalkylammonium ion, and an ion exchange resin functionalized with quaternary amine groups; and

X.sup.- =carbonate, bicarbonate, hydroxide, and formate.

15. The kit of claim 6, wherein in R', C includes a radioactive isotope of carbon.
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