[3 H] MFZ 2-12: A Novel Radioligand for the Dopamine Transporter

AH Newman, MF Zou, JV Ferrer, JA Javitch

Index: Newman, Amy Hauck; Zou, Mu-Fa; Ferrer, Jasmine V.; Javitch, Jonathan A. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 13 p. 1659 - 1661

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Citation Number: 8

Abstract

In an effort to develop a tritiated dopamine transporter radioligand with higher affinity than the widely used [3H] WIN 35,428, we have synthesized [3H] 2β-carbomethoxy-3β-(3′, 4′- dichlorophenyl) tropane ([3H] 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 ...