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Chemical Compound Review

Talsupram     3-(7,7-dimethyl-9-phenyl-8...

Synonyms: Talsupramum, CHEMBL52247, SureCN114515, CHEBI:180836, AC1L1OUE, ...
 
 
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High impact information on Talsupram

  • Neither talsupram, a noradrenergic transport inhibitor, nor prazosin, a noradrenergic antagonist selective for alpha-1 receptors, systematically altered the cocaine-like DS effects of heroin at doses that enhanced (talsupram) or attenuated (prazosin) the DS effects of cocaine [1].
  • The specific 5-HT- and NA-uptake inhibitors citalopram and talsupram, respectively, were ineffective in all rat models.(ABSTRACT TRUNCATED AT 250 WORDS)[2]
  • The two most promising compounds, talopram and talsupram, were radiolabeled with carbon-11 and evaluated through biodistribution studies in rats and PET imaging studies in a rhesus monkey [3].
  • Desipramine (DMI), talopram and talsupram, three of the most potent norepinephrine transporter (NET) inhibitors reported to date, were radiolabeled in high yields and at high specific radioactivity (58-75 GBq/micromol) by the methylation of nor-precursors with [C-11]methyl triflate [4].

References

  1. Cocaine-like discriminative stimulus effects of heroin: modulation by selective monoamine transport inhibitors. Rowlett, J.K., Platt, D.M., Spealman, R.D. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  2. Pharmacology in vivo of the phenylindan derivative, Lu 19-005, a new potent inhibitor of dopamine, noradrenaline and 5-hydroxytryptamine uptake in rat brain. Arnt, J., Christensen, A.V., Hyttel, J. Naunyn Schmiedebergs Arch. Pharmacol. (1985) [Pubmed]
  3. Synthesis and biological evaluation of [11C]talopram and [11C]talsupram: candidate PET ligands for the norepinephrine transporter. McConathy, J., Owens, M.J., Kilts, C.D., Malveaux, E.J., Camp, V.M., Votaw, J.R., Nemeroff, C.B., Goodman, M.M. Nucl. Med. Biol. (2004) [Pubmed]
  4. Synthesis and positron emission tomography evaluation of three norepinephrine transporter radioligands: [C-11]desipramine, [C-11]talopram and [C-11]talsupram. Schou, M., Sóvágó, J., Pike, V.W., Gulyás, B., Bøgesø, K.P., Farde, L., Halldin, C. Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging. (2006) [Pubmed]
 
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