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Spice drugs are more than harmless herbal blends: A review of the pharmacology and toxicology of synthetic cannabinoids
Phase I Hydroxylated Metabolites of the K2 Synthetic Cannabinoid JWH-018 Retain In Vitro and In Vivo Cannabinoid 1 Receptor Affinity and Activity
- L. Brents, E. Reichard, S. Zimmerman, J. Moran, W. Fantegrossi, P. Prather
- Biology, ChemistryPloS one
- 6 July 2011
This study proposes that K2's high adverse effect occurrence is due, at least in part, to distinct JWH-018 metabolite activity at the cannabinoid 1 receptor (CB1R), and suggests that metabolites of most drugs, but not the carboxy metabolite, retain in vitro and in vivo activity at CB1Rs.
Distinct pharmacology and metabolism of K2 synthetic cannabinoids compared to Δ(9)-THC: mechanism underlying greater toxicity?
Cytochrome P450-Mediated Oxidative Metabolism of Abused Synthetic Cannabinoids Found in K2/Spice: Identification of Novel Cannabinoid Receptor Ligands
- Krishna C Chimalakonda, K. Seely, J. Moran
- Chemistry, BiologyDrug Metabolism and Disposition
- 1 November 2012
Test the hypothesis that JWH-018 and its fluorinated counterpart AM2201 are subject to cytochrome P450 (P450)-mediated oxidation, forming potent hydroxylated metabolites that retain significant affinity and activity at the cannabinoid 1 (CB1) receptor.
Monohydroxylated metabolites of the K2 synthetic cannabinoid JWH-073 retain intermediate to high cannabinoid 1 receptor (CB1R) affinity and exhibit neutral antagonist to partial agonist activity.
Severe Toxicity Following Synthetic Cannabinoid Ingestion
- J. Lapoint, L. James, C. Moran, L. Nelson, R. Hoffman, J. Moran
- MedicineClinical toxicology
- 1 October 2011
Ingestion of JWH-018 can produce seizures and tachyarrhythmias, and Clinicians, lawmakers, and the general public need to be aware of the potential for toxicity associated with synthetic cannabinoid use.
Marijuana-based drugs: innovative therapeutics or designer drugs of abuse?
The K2/Spice "phenomenon" provides a context for considering whether marijuana-based drugs will truly provide innovative therapeutics or merely perpetuate drug abuse.
Characterization of Human Hepatic and Extrahepatic UDP-Glucuronosyltransferase Enzymes Involved in the Metabolism of Classic Cannabinoids
This study test the hypothesis that there are specific human UGTs responsible for classic cannabinoid metabolism and finds that CBN was the most recognized substrate as evidenced by activities from hepatic UGT1A9 and extrahepatic U GT1A7, UGT 1A8, and UGT2A10.
Quantitative measurement of JWH-018 and JWH-073 metabolites excreted in human urine.
A liquid chromatography-tandem mass spectrometry method for measuring urinary concentrations of JWH-018,JWH-073, and several potential metabolites of each is validated, clinically validating the LC-MS/MS assay for detecting and quantifying aminoalkylindole metabolites.