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Chemical Compound Review

beta-Cft     methyl(1R,2S,3S,5S)-3-(4- fluorophenyl)-8...

Synonyms: CHEMBL1944829, SureCN1573076, AC1L2XYH, AR-1J6265, KB-205331, ...
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Disease relevance of beta-Cft

  • In the present study, we address this issue by examining the inhibition by mazindol of the binding of [3H]WIN 35,428 ([3H]2beta-carbomethyoxy-3beta-(4-fluorophenyl)-tropane), a phenyltropane analog of cocaine, and the inhibition by WIN 35,428 of [3H]mazindol binding to the cloned human dopamine transporter expressed in C6 glioma cells [1].

Psychiatry related information on beta-Cft


High impact information on beta-Cft

  • To establish that DA deficiency is present in LND, the ligand WIN-35,428, which binds to DA transporters, was used to estimate the density of DA-containing neurons in the caudate and putamen of six patients with classic LND [3].
  • The DAT inhibitor, WIN-35,428, protected completely against METH-induced DA neurotoxicity in AMIL pretreated animals, suggesting that the potentiating effects of AMIL require a METH/DAT interaction [4].
  • The K+ IC50 for inhibiting dopamine or WIN 35,428 binding increased linearly with [Na+], indicating a K(D,Na+) of 30-44 mM and a K(D,K+) of 13-16 mM for this cation site [5].
  • In comparison with GBR 12909 [1-[2-(bis(4-fluorophenyl)methoxy)ethyl]-4-(3-phenylpropyl)piperazine ] and WIN 35,428 [3beta-(p-fluorophenyl)-2beta-carbomethoxytropane] binding, these two novel N-analogues were slightly more potent and far more selective for the DAT [6].
  • Brain dopamine transporter binding sites were quantified by in vitro autoradiography using [3H] WIN 35,428 as ligand [2].

Biological context of beta-Cft

  • The results are discussed in the context of transporter loss from the cell surface, or a model with phosphorylation affecting the shared dopamine and WIN 35,428 binding domain on the transporter as well as affecting a part of the dopamine binding domain lying outside that for WIN 35,428 [7].
  • RESULTS: [3H] Win 35,428 saturation binding assays and DAT immunoblots revealed statistically significant differences in DAT expression attributable to DAT1 genotype [8].

Anatomical context of beta-Cft

  • Modeling of the pH dependence of the binding of WIN 35,428 to the dopamine transporter in rat striatal membranes: is the bioactive form positively charged or neutral [9]?

Associations of beta-Cft with other chemical compounds


Gene context of beta-Cft


Analytical, diagnostic and therapeutic context of beta-Cft


  1. WIN 35,428 and mazindol are mutually exclusive in binding to the cloned human dopamine transporter. Xu, C., Reith, M.E. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  2. Chronic psychosocial stress reduces the density of dopamine transporters. Isovich, E., Mijnster, M.J., Flügge, G., Fuchs, E. Eur. J. Neurosci. (2000) [Pubmed]
  3. Dopamine transporters are markedly reduced in Lesch-Nyhan disease in vivo. Wong, D.F., Harris, J.C., Naidu, S., Yokoi, F., Marenco, S., Dannals, R.F., Ravert, H.T., Yaster, M., Evans, A., Rousset, O., Bryan, R.N., Gjedde, A., Kuhar, M.J., Breese, G.R. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  4. Inhibitors of Na(+)/H(+) and Na(+)/Ca(2+) exchange potentiate methamphetamine-induced dopamine neurotoxicity: possible role of ionic dysregulation in methamphetamine neurotoxicity. Callahan, B.T., Cord, B.J., Yuan, J., McCann, U.D., Ricaurte, G.A. J. Neurochem. (2001) [Pubmed]
  5. Modeling of the interaction of Na+ and K+ with the binding of dopamine and [3H]WIN 35,428 to the human dopamine transporter. Li, L.B., Reith, M.E. J. Neurochem. (1999) [Pubmed]
  6. Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter. Dutta, A.K., Xu, C., Reith, M.E. J. Med. Chem. (1998) [Pubmed]
  7. Regulation of the functional activity of the human dopamine transporter by protein kinase C. Zhang, L., Coffey, L.L., Reith, M.E. Biochem. Pharmacol. (1997) [Pubmed]
  8. The variable number of tandem repeats element in DAT1 regulates in vitro dopamine transporter density. VanNess, S.H., Owens, M.J., Kilts, C.D. BMC Genet. (2005) [Pubmed]
  9. Modeling of the pH dependence of the binding of WIN 35,428 to the dopamine transporter in rat striatal membranes: is the bioactive form positively charged or neutral? Xu, C., Reith, M.E. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  10. Cocaine receptors labeled by [3H]2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane. Madras, B.K., Spealman, R.D., Fahey, M.A., Neumeyer, J.L., Saha, J.K., Milius, R.A. Mol. Pharmacol. (1989) [Pubmed]
  11. Altropane, a SPECT or PET imaging probe for dopamine neurons: I. Dopamine transporter binding in primate brain. Madras, B.K., Meltzer, P.C., Liang, A.Y., Elmaleh, D.R., Babich, J., Fischman, A.J. Synapse (1998) [Pubmed]
  12. Translocation of dopamine and binding of WIN 35,428 measured under identical conditions in cells expressing the cloned human dopamine transporter. Reith, M.E., Xu, C., Zhang, L., Coffey, L.L. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  13. Dopamine terminal loss and onset of motor symptoms in MPTP-treated monkeys: a positron emission tomography study with 11C-CFT. Wüllner, U., Pakzaban, P., Brownell, A.L., Hantraye, P., Burns, L., Shoup, T., Elmaleh, D., Petto, A.J., Spealman, R.D., Brownell, G.L. Exp. Neurol. (1994) [Pubmed]
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