publication . Other literature type . Article . 2015

Effects of Bioisosteric Fluorine in Synthetic Cannabinoid Designer Drugs JWH-018, AM-2201, UR-144, XLR-11, PB-22, 5F-PB-22, APICA, and STS-135

Samuel D. Banister; Jordyn Stuart; Richard C. Kevin; Amelia R. Edington; Mitchell Longworth; Shane M. Wilkinson; Corinne Beinat; Alexandra S. Buchanan; David E. Hibbs; Michelle Glass; ...
Open Access
  • Published: 08 May 2015
  • Publisher: American Chemical Society (ACS)
Abstract
Synthetic cannabinoid (SC) designer drugs featuring bioisosteric fluorine substitution are identified by forensic chemists and toxicologists with increasing frequency. Although terminal fluorination of N-pentyl indole SCs is sometimes known to improve cannabinoid type 1 (CB1) receptor binding affinity, little is known of the effects of fluorination on functional activity of SCs. This study explores the in vitro functional activities of SC designer drugs JWH-018, UR-144, PB-22, and APICA, and their respective terminally fluorinated analogues AM-2201, XLR-11, 5F-PB-22, and STS-135 at human CB1 and CB2 receptors using a FLIPR membrane potential assay. All compounds...
Persistent Identifiers
Subjects
free text keywords: Cell Biology, Biochemistry, Physiology, Cognitive Neuroscience, General Medicine, THC, AM-2201, XLR-11, JWH-018, medicine.drug, medicine, APICA, PB-22, Cannabinoid receptor, Designer drug, medicine.drug_class, Chemistry, Cannabinoid receptor type 2, Stereochemistry, UR-144, Cannabinoid, medicine.medical_treatment
Funded by
EC| INMIND
Project
INMIND
Imaging of Neuroinflammation in Neurodegenerative Diseases
  • Funder: European Commission (EC)
  • Project Code: 278850
  • Funding stream: FP7 | SP1 | HEALTH
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