Structure-Activity Relationships of Substituted Cathinones, with Transporter Binding, Uptake, and Release

• Published in: The Journal of pharmacology and experimental therapeutics Vol. 360; no. 1; pp. 33 - 47
• Main Authors: Eshleman, Amy J., Wolfrum, Katherine M., Reed, John F., Kim, Sunyoung O., Swanson, Tracy, Johnson, Robert A., Janowsky, Aaron
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.01.2017; The American Society for Pharmacology and Experimental Therapeutics
• Subjects: Alkaloids - chemistry; Alkaloids - pharmacology; Biological Transport - drug effects; Humans; Neuropharmacology; Neurotransmitter Agents - metabolism; Neurotransmitter Transport Proteins - metabolism; Protein Binding - drug effects; Structure-Activity Relationship; 4-MePPP; 3,4-MDPPP; ethylone; 4-Cl MCAT; RTI-55; pentedrone; AUC; MDMA; 3-F MCAT; 4-F MCAT; 3,4-MDPBP; PV-8; ANOVA; ICSS; α-PBP; pentylone; MDAI; hSERT; 5-MeO-methylone; 4-MEC; hNET; 4-MeO-α-PVP; 4-Br MCAT; α-PHP; butylone; METH; α-PVT; 4-FA; MCAT; α-PPP; HEK; PCA; SERT; α-PVP; DAT; NE; MDPV; 5-HT; NET; DA; hDAT

Synthetic cathinones are components of “bath salts” and have physical and psychologic side effects, including hypertension, paranoia, and hallucinations. Here, we report interactions of 20 “bath salt” components with human dopamine, serotonin, and norepinephrine transporters [human dopamine transpor...