Technepine: A high-affinity99mtechnetium probe to label the dopamine transporter in brain by SPECT imaging

Madras, Bertha K.; Jones, Alun G.; Mahmood, Ashfaq; Zimmerman, R.E.; Garada, B; Holman, B. Leonard; Davison, Alan; Blundell, Paul; Meltzer, Peter C.

doi:10.1002/(sici)1098-2396(199603)22:3<239::aid-syn6>3.0.co;2-d

Cited by 67 publications

(37 citation statements)

References 29 publications

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“…The corresponding rhenium analogue displayed an inhibition constant (K i ) of 14.1 nM toward DAT. Madras and co-workers have reported a similar result with one of a series of N 2 S 2 chelate analogues of the fluorophenyltropane CFT conjugated at the N-8 position (10). Together, these studies demonstrate that technetium-99m can be incorporated into a radiotracer that has a high affinity for the target site, crosses the blood-brain barrier, and concentrates in the appropriate target regions in the brain.…”

Section: Introductionmentioning

confidence: 68%

Synthesis of Cyclopentadienyltricarbonyl Rhenium Phenyltropanes by Double Ligand Transfer: Organometallic Ligands for the Dopamine Transporter

et al. 2001

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Cyclopentadienyltricarbonyl rhenium (CpRe(CO)(3)) systems can be prepared from ferrocenes and perrhenate by a double ligand transfer (DLT) reaction that gives reasonable yields and shows excellent functional group tolerance. We used this reaction for the direct preparation of CpRe(CO)(3)-phenyltropane conjugates. Such agents, when labeled with technetium-99m, might function as imaging agents for the dopamine transporter (DAT) system that would be useful for assessing the onset and severity of Parkinson's disease. Of the CpRe(CO)(3)-tropane conjugates prepared by the DLT reaction (as well as other analogues prepared by related methods), those substituted at the N-8 position seem most promising; their affinity for the DAT in all cases was high, and their ferrocene precursors for the DLT reaction can be prepared in a convenient manner. By contrast, the 3 beta-conjugates were poor DAT binders. The modular nature of these systems offers considerable flexibility that could be used to improve the binding characteristics of these compounds further.

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Section: Introductionmentioning

confidence: 68%

Synthesis of Cyclopentadienyltricarbonyl Rhenium Phenyltropanes by Double Ligand Transfer: Organometallic Ligands for the Dopamine Transporter

et al. 2001

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“…Imaging agents that label the DAT non-invasively have enabled quantification of DAT density in living brain. 6,10,68,69 As described previously, contradictory data were reported when comparing individuals harboring 9-and/or 10-repeat length alleles. 38,43 As ADHD has a small but significant association with DAT 10-repeat length alleles, several groups investigated whether DAT levels in ADHD brains deviate from the normal range.…”

Section: Discussionmentioning

confidence: 99%

Polymorphisms in the 3′-untranslated region of human and monkey dopamine transporter genes affect reporter gene expression

Miller

2002

Mol Psychiatry

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“…Cells were grown in 145-mm untreated tissue culture dishes (Greiner America, Inc., Lake Mary, FL) in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum, 100 U ml −1 penicillin, 100 μg streptomycin, and 0.1 mM nonessential amino acids (all from Life Technologies, Rockville, MD), at 5% CO 2 in a 37°C water-jacketed incubator. (Madras et al 1989b(Madras et al , 1996Goulet et al 2001). Experiments were terminated by centrifugation and aspiration of the supernatant as described above.…”

Section: Methodsmentioning

confidence: 99%

MDMA (Ecstasy) and human dopamine, norepinephrine, and serotonin transporters: implications for MDMA-induced neurotoxicity and treatment

2005

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Rationale: 3,4-Methylenedioxymethamphetamine (MDMA, designated as "Ecstasy" if illicitly marketed in tablet form) induces significant decrements in neuronal serotonin (5-HT) markers in humans, nonhuman primates, and rats as a function of dosing and dosing regimen. In rats, MDMA-mediated effects are attributed, in part, to selective high-affinity transport of MDMA The affinity of MDMA for the human SERT in transfected cells does not clarify the apparent selective toxicity of MDMA for serotonin neurons, although conceivably, its higher efficacy for stimulating 5-HT release may be a distinguishing factor. The findings highlight the need to investigate MDMA effects in DAT-, SERT-, and NET-expressing neurons in the primate brain and the therapeutic potential of NET or DAT inhibitors, in addition to SERT-selective inhibitors, for alleviating the pharmacological effects of MDMA.

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Technepine: A high-affinity99mtechnetium probe to label the dopamine transporter in brain by SPECT imaging

Cited by 67 publications

References 29 publications

Synthesis of Cyclopentadienyltricarbonyl Rhenium Phenyltropanes by Double Ligand Transfer: Organometallic Ligands for the Dopamine Transporter

Synthesis of Cyclopentadienyltricarbonyl Rhenium Phenyltropanes by Double Ligand Transfer: Organometallic Ligands for the Dopamine Transporter

Polymorphisms in the 3′-untranslated region of human and monkey dopamine transporter genes affect reporter gene expression

MDMA (Ecstasy) and human dopamine, norepinephrine, and serotonin transporters: implications for MDMA-induced neurotoxicity and treatment

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