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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  <identifier identifierType="URL"></identifier>
      <creatorName>Stathis, M.</creatorName>
      <creatorName>Scheffel, U.</creatorName>
      <creatorName>Lever, S. Z.</creatorName>
      <givenName>S. Z.</givenName>
      <creatorName>Boja, J. W.</creatorName>
      <givenName>J. W.</givenName>
      <creatorName>Kuhar, M. J.</creatorName>
      <givenName>M. J.</givenName>
      <creatorName>Carroll, F. I.</creatorName>
      <givenName>F. I.</givenName>
    <title>Rate of binding of various inhibitors at the dopamine transporter in vivo</title>
    <date dateType="Issued">1995-06-01</date>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
    <alternateIdentifier alternateIdentifierType="url"></alternateIdentifier>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1007/bf02245852</relatedIdentifier>
    <rights rightsURI="">Creative Commons Zero v1.0 Universal</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
    <description descriptionType="Abstract">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</description>
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