Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 13, Pages 1659-1661Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00271-2
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- NIDA NIH HHS [DA11495] Funding Source: Medline
- NIMH NIH HHS [MH57324] Funding Source: Medline
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In an effort to develop a tritiated dopamine transporter radioligand with higher affinity than the widely used [H-3]WIN 35,428, we have synthesized [H-3]3 beta -carbomethoxy-3 beta-(3 ' .4 ' -dichloroph ([H-3]MFZ 2 12). Unlabeled MFZ 2-12 and the N-demethylated intermediate (MFZ 2-13) inhibited dopamine uptake by the human dopamine transporter with IC50's of 1.1 and 1.4 nM, respectively. The N-nor-intermediate (MFZ 2-13) was treated with CT,I resulting in [H-3]MFZ 2-12, S.A. = 80 Ci/mmol). [H-3]MFZ 2-12 reversibly bound with a KD of 2.8 nM to human dopamine transporter expressed heterologously in EM4 cells. Published by Elsevier Science Ltd.
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