Journal article Open Access

Rate of binding of various inhibitors at the dopamine transporter in vivo

Stathis, M.; Scheffel, U.; Lever, S. Z.; Boja, J. W.; Kuhar, M. J.; Carroll, F. I.


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  <dc:creator>Stathis, M.</dc:creator>
  <dc:creator>Scheffel, U.</dc:creator>
  <dc:creator>Lever, S. Z.</dc:creator>
  <dc:creator>Boja, J. W.</dc:creator>
  <dc:creator>Kuhar, M. J.</dc:creator>
  <dc:creator>Carroll, F. I.</dc:creator>
  <dc:date>1995-06-01</dc:date>
  <dc:description>The rate of entry of drugs into brain is thought to be a factor in their abuse liability. In this investigation, we have examined the rate of entry and binding at dopamine transporters in mouse striatum for a variety of dopamine transporter inhibitors. The method utilized was based on measuring the displacement of3H-WIN 35,428 from striatal dopamine transporter sites in vivo at different times. Eleven cocaine analogs (RTI-31, RTI-32, RTI-51, RTI-55, RTI-113, RTI-114, RTI-117, RTI-120, RTI-121, WIN 35,065-2, and WIN 35,428) as well as other dopamine uptake site blockers (bupropion, nomifensine, and methylphenidate) were compared with (−) cocaine for their rates of displacement of3H-WIN 35,428 binding in vivo. The drugs that displayed the fastest occupancy rates were bupropion, (−) cocaine, nomifensine, and methylphenidate. RTI-51, RTI-121, RTI-114, RTI-117, RTI-120, RTI-32, RTI-55, and RTI-113, showed intermediate rates, whereas RTI-31, WIN 35,065-2, and WIN 35,428 exhibited the slowest rates of displacement. While many of the cocaine analogs have proven to be behaviorally and pharmacologically more potent than (−) cocaine, their rates of entry and binding site occupancy were slower than that for (−) cocaine. Earliest times of transporter occupancy by the different drugs were correlated (although weakly) with their degree of lipophilicity (r=0.59;P</dc:description>
  <dc:identifier>https://zenodo.org/record/1232524</dc:identifier>
  <dc:identifier>10.1007/bf02245852</dc:identifier>
  <dc:identifier>oai:zenodo.org:1232524</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>http://creativecommons.org/publicdomain/zero/1.0/legalcode</dc:rights>
  <dc:title>Rate of binding of various inhibitors at the dopamine transporter in vivo</dc:title>
  <dc:type>info:eu-repo/semantics/article</dc:type>
  <dc:type>publication-article</dc:type>
</oai_dc:dc>
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