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.


DataCite XML Export

<?xml version='1.0' encoding='utf-8'?>
<resource xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xmlns="http://datacite.org/schema/kernel-4" xsi:schemaLocation="http://datacite.org/schema/kernel-4 http://schema.datacite.org/meta/kernel-4.1/metadata.xsd">
  <identifier identifierType="URL">https://zenodo.org/record/1232524</identifier>
  <creators>
    <creator>
      <creatorName>Stathis, M.</creatorName>
      <givenName>M.</givenName>
      <familyName>Stathis</familyName>
    </creator>
    <creator>
      <creatorName>Scheffel, U.</creatorName>
      <givenName>U.</givenName>
      <familyName>Scheffel</familyName>
    </creator>
    <creator>
      <creatorName>Lever, S. Z.</creatorName>
      <givenName>S. Z.</givenName>
      <familyName>Lever</familyName>
    </creator>
    <creator>
      <creatorName>Boja, J. W.</creatorName>
      <givenName>J. W.</givenName>
      <familyName>Boja</familyName>
    </creator>
    <creator>
      <creatorName>Kuhar, M. J.</creatorName>
      <givenName>M. J.</givenName>
      <familyName>Kuhar</familyName>
    </creator>
    <creator>
      <creatorName>Carroll, F. I.</creatorName>
      <givenName>F. I.</givenName>
      <familyName>Carroll</familyName>
    </creator>
  </creators>
  <titles>
    <title>Rate of binding of various inhibitors at the dopamine transporter in vivo</title>
  </titles>
  <publisher>Zenodo</publisher>
  <publicationYear>1995</publicationYear>
  <dates>
    <date dateType="Issued">1995-06-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://zenodo.org/record/1232524</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1007/bf02245852</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://creativecommons.org/publicdomain/zero/1.0/legalcode">Creative Commons Zero v1.0 Universal</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <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>
  </descriptions>
</resource>
21
11
views
downloads
Views 21
Downloads 11
Data volume 10.5 MB
Unique views 21
Unique downloads 11

Share

Cite as