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Claims for Patent: 5,310,912

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Claims for Patent: 5,310,912

Title: Iodinated 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=a C.sub.n H.sub.2n+1 group where n=0-6, an alkenyl group, a monofluoroalkyl group including .sup.n F where n=18 or 19, or a .sup.m C.sub.n H.sub.2n+1 group where n=1-6 and where m=11 or 14 for at least one .sup.m C; R'=a C.sub.n H.sub.2n+1 group where n=0-6, a p-iodophenylmethyl group, a p-iodophenylethyl group, a phenylmethyl group, or a phenylethyl group; X=an isotope of F, an isotope of Cl, an isotope of Br, an isotope of I, CH.sub.3, or Sn(R".sub.1 R".sub.2 R".sub.3); R".sub.1 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.2 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; R".sub.3 =a C.sub.n H.sub.2n+1 group where n=1-6, or an aryl group; and Y=H only if X is an isotope of I, or R' is a p-iodophenylmethyl group, or R' is a p-iodophenylethyl group, else Y=an isotope of I. Related analogs are also provided. Additionally, a precursor of a radiolabled neuroprobe and a kit for preparing the iodinated neuroprobe are provided.
Inventor(s): Neumeyer; John L. (Wayland, MA), Milius; Richard A. (Boston, MA), Innis; Robert B. (Hamden, CT)
Assignee: Research Biochemicals Limited Partnership (Natick, MA)
Application Number:07/841,617
Patent Claims: 1. An iodinated neuroprobe for mapping monoamine reuptake sites, the iodinated neuroprobe being of the formula: ##STR4## wherein R=a monofluoroalkyl group including .sup.n F where n=18 or 19;

R'=a C.sub.n H.sub.2n+1 group where n=0-6;

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

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

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

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

Y=H.

2. The iodinated neuroprobe of claim 1 wherein X=.sup.123 I.

3. The iodinated neuroprobe of claim 1 wherein X=.sup.125 I.

4. The iodinated neuroprobe of claim 1 wherein X=.sup.131 I.

5. An iodinated neuroprobe for mapping monoamine reuptake sites, the iodinated neuroprobe being of the formula: ##STR5## wherein R=a monofluoroalkyl group including .sup.n F where n=18 or 19;

R'=a C.sub.n H.sub.2n+1 group where n=0-6;

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

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

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

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

Y=H.

6. The iodinated neuroprobe of claim 5 wherein X=.sup.123 I.

7. The iodinated neuroprobe of claim 5 wherein X=.sup.125 I.

8. The iodinated neuroprobe of claim 5 wherein X=.sup.131 I.
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