Pharmacological characterization of designer cathinones in vitro

Background and Purpose Designer β‐keto amphetamines (e.g. cathinones, ‘bath salts’ and ‘research chemicals’) have become popular recreational drugs, but their pharmacology is poorly characterized. Experimental Approach We determined the potencies of cathinones to inhibit DA , NA and 5‐ HT transport into transporter‐transfected HEK 293 cells, DA and 5‐ HT efflux from monoamine‐preloaded cells, and monoamine receptor binding affinity. Key Results Mephedrone, methylone, ethylone, butylone and naphyrone acted as non‐selective monoamine uptake inhibitors, similar to cocaine. Mephedrone, methylone, ethylone and butylone also induced the release of 5‐ HT , similar to 3,4‐methylenedioxymethamphetamine ( MDMA ,…

• NS
  National Science Foundation
• UB
  Universität Basel
• SN
  Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung