ArticleThe AAPS journal2015
CYP3A4 Mediates Oxidative Metabolism of the Synthetic Cannabinoid AKB-48.
Article in The AAPS journal, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 43 citations in OpenAlex.
- The resurgence of synthetic cannabinoid receptor agonists as adulterants in the Era of Cannabis legalization: Lessons from prior epidemics and clinical implications.Neuroscience and biobehavioral reviews · 2025Review
- Characterisation of AMB-FUBINACA metabolism and CBForensic toxicology · 2023Article
- Synthetic Cannabinoid-Related Deaths in England, 2012-2019.Cannabis and cannabinoid research · 2022Article
- Phase I In Vitro Metabolic Profiling of the Synthetic Cannabinoid Receptor Agonists CUMYL-THPINACA and ADAMANTYL-THPINACA.Metabolites · 2021Article
- Pharmacology and adverse effects of new psychoactive substances: synthetic cannabinoid receptor agonists.Archives of pharmacal research · 2021Review
- Significance of Competing Metabolic Pathways for 5F-APINACA Based on Quantitative Kinetics.Molecules (Basel, Switzerland) · 2020Article
- Metabolism, CB1 cannabinoid receptor binding and in vivo activity of synthetic cannabinoid 5F-AKB48: Implications for toxicity.Pharmacology, biochemistry, and behavior · 2020Article
- Metabolic Profiling of a CB2 Agonist, AM9338, Using LC-MS and Microcoil-NMR: Identification of a Novel Dihydroxy Adamantyl Metabolite.Frontiers in pharmacology · 2020Article
- In Vitro Inhibitory Effects of APINACA on Human Major Cytochrome P450, UDP-Glucuronosyltransferase Enzymes, and Drug Transporters.Molecules (Basel, Switzerland) · 2019Article
- Synthetic Cannabinoid Hydroxypentyl Metabolites Retain Efficacy at Human Cannabinoid Receptors.The Journal of pharmacology and experimental therapeutics · 2019Article
- Pharmacological and Behavioral Effects of the Synthetic Cannabinoid AKB48 in Rats.Frontiers in neuroscience · 2019Article
- Synthetic Pot: Not Your Grandfather's Marijuana.Trends in pharmacological sciences · 2017Review
- In vitro and in vivo human metabolism of a new synthetic cannabinoid NM-2201 (CBL-2201).Forensic toxicology · 2017Article
- Effect of the novel synthetic cannabinoids AKB48 and 5F-AKB48 on "tetrad", sensorimotor, neurological and neurochemical responses in mice. In vitro and in vivo pharmacological studies.Psychopharmacology · 2016Article
- Emerging drugs of abuse: current perspectives on synthetic cannabinoids.Substance abuse and rehabilitation · 2015Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Synthetic cannabinoid designer drugs have emerged as drugs of abuse during the last decade, and acute intoxication cases are documented in the scientific literature. Synthetic cannabinoids are extensively metabolized, but our knowledge of the involved enzymes is limited. Here, we investigated the metabolism of N-(1-adamantyl)-1-pentyl-1H-indazole-3-carboxamide (AKB-48), a compound identified in herbal blends from 2012 and onwards. We screened for metabolite formation using a panel of nine recombinant cytochrome P450 (CYP) enzymes (CYP1A2, 2B6, 2C8, 2C9, 2C18, 2C19, 2D6, 2E1, and 3A4) and compared the formed metabolites to human liver microsomal (HLM) incubations with specific inhibitors against CYP2D6, 2C19, and 3A4, respectively. The data reported here demonstrate CYP3A4 to be the major CYP enzyme responsible for the oxidative metabolism of AKB-48, preferentially performing the oxidation on the adamantyl moiety. Genetic polymorphisms are likely not important with regard to toxicity given the major involvement of CYP3A4. Adverse drug-drug interactions (DDIs) could potentially occur in cases with co-intake of strong CYP3A4 inhibitors, e.g., HIV antivirals and azole antifungal agents.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.