MDPV>α-PPP≈MDPBP>MDPPP>cocaine.ComparisonsofthemaximumnumberofinfusionsobtainedunderaPRscheduleofreinforcement(α-PVP>MDPV>α-PPP>MDPBP≈MDPPP>cocaine)andtheessentialvalueobtainedforeachdrugindemandanalyses(α-PVP>MDPV>α-PPP≈MDPBP≈MDPPP>cocaine)suggestrelativereinforcingeffectivenessisrelatedtoDAT/SERTselectivity.CONCLUSIONThesedataprovideevidencethatDAT/SERTselectivityaccountsforselectsyntheticcathinonesfunctioningasmoreeffectivereinforcersthancocaineandmaypredicttheabuse-relatedeffectsofnovelsyntheticcathinonesinhumans.">
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Abuse-relatedeffectsofsyntheticcathinones:importanceofDAT/SERTrelationships

摘要： OBJECTIVEWidespreadabuseofsyntheticcathinonesfoundinbathsaltspreparationshasresultedinregulationofsomecathinonesinternationally.Chemistsskirttheselawsbyalteringthechemicalstructuresoffirst-generationcathinones(ie,MDPV,methylone,andmephedrone),resultinginsecond-generationcathinones(eg,α-PVP,α-PPP,MDPPP,andMDPBP).AlthoughMDPVisamoreeffectivereinforcerthancocaine,littleisknownaboutthereinforcingeffectivenessofsecondgenerationcathinones.TotestthehypothesisthatsyntheticcathinoneswithhigherselectivityforDATrelativetoSERTaremoreeffectivereinforcers.METHODSMonoaminetransporterinhibitionwasdeterminedusingsynaptosomespreparedfromratbrains.Therelativereinforcingeffectivenessofintravenouslyself-administeredMDPV,MDPBP,MDPPP,α-PVP,α-PPP,andcocaineweredirectlycomparedthroughevaluationsof(1)dose-responsecurvesunderaprogressiveratio(PR)scheduleofreinforcementand(2)demandcurvesobtainedforeachdruginmaleSprague-Dawleyrats.RESULTSRankorderselectivityforDAT/SERTwasα-PVP>MDPV>α-PPP≈MDPBP>MDPPP>cocaine.ComparisonsofthemaximumnumberofinfusionsobtainedunderaPRscheduleofreinforcement(α-PVP>MDPV>α-PPP>MDPBP≈MDPPP>cocaine)andtheessentialvalueobtainedforeachdrugindemandanalyses(α-PVP>MDPV>α-PPP≈MDPBP≈MDPPP>cocaine)suggestrelativereinforcingeffectivenessisrelatedtoDAT/SERTselectivity.CONCLUSIONThesedataprovideevidencethatDAT/SERTselectivityaccountsforselectsyntheticcathinonesfunctioningasmoreeffectivereinforcersthancocaineandmaypredicttheabuse-relatedeffectsofnovelsyntheticcathinonesinhumans. ... （共1頁）

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