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AM-2201 [CAS Number 335161-24-5] is a potent synthetic cannabinoid receptor agonist. It is one of the most commonly detected synthetic cannabinoids and is a fluorinated analogue of JWH-018. It is also considered a designer drug for recreational use. AM-2201 is a controlled substance. Buy AM 2201 online, AM 2201 drug, AM 2201 for sale, AM 2201 chemical, where to buy AM 2201. AM-2201 is available as a reference material (bulk powder and/or solution) and as a calibrated, ready-to-use certified reference material (CRM). Designed for qualitative and quantitative protocols, this product can be used for forensics, toxicology, research, and other chemical/biochemical analysis applications.
A synthetic cannabanoid that is very potent. Active doses start at around 250ug’s. Please be cautious with this substance. It has also been noted that it can cause convulsions.
AM-2201 is a synthetic cannabinoid that acts as a potent agonist at cannabinoid receptors and its abuse has increased. However, there are no reports of the inhibitory effect of AM-2201 on human cytochrome P450 (CYP) or uridine 5′-diphospho-glucuronosyltransferase (UGT) enzymes. We evaluated the inhibitory effect of AM-2201 on the activities of eight major human CYPs (1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4) and six major human UGTs (1A1, 1A3, 1A4, 1A6, 1A9, and 2B7) enzymes in pooled human liver microsomes using liquid chromatography–tandem mass spectrometry to investigate drug interaction potentials of AM-2201. AM-2201 potently inhibited CYP2C9-catalyzed diclofenac 4′-hydroxylation, CYP3A4-catalyzed midazolam 1′-hydroxylation, UGT1A3-catalyzed chenodeoxycholic acid 24-acyl-glucuronidation, and UGT2B7-catalyzed naloxone 3-glucuronidation with IC50 values of 3.9, 4.0, 4.3, and 10.0 µM, respectively, and showed mechanism-based inhibition of CYP2C8-catalyzed amodiaquine N-deethylation with a Ki value of 2.1 µM. It negligibly inhibited CYP1A2, CYP2A6, CYP2B6, CYP2C19, CYP2D6, UGT1A1, UGT1A4, UGT1A6, and UGT1A9 activities at 50 μM in human liver microsomes. These in vitro results strongly inhibit the enzymatic activities of CYP2C8, CYP2C9, CYP3A4, UGT1A3, and UGT2B7, thus AM-2201 should be evaluated in vivo for potential pharmacokinetic drug interactions. indicates that
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AM-2201; cytochrome P450 inhibition; UDP glucuronosyltransferase inhibition; human liver microsomes; drug interactions
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Synthetic cannabinoids are a group of substances with effects functionally similar to Δ9-tetrahydrocannabinol (THC), responsible for the main psychoactive effects of cannabis, and are generally classified as cannabinoid receptor type 1 (CB1) or 2 ( CB2) [1] . The synthetic cannabinoid JWH-018 was first discovered in 2008 in an herbal smoking blend called Spice. Currently, 160 synthetic cannabinoids are monitored by the European Center for the Surveillance of Drugs and Drug Addiction (EMCDDA) through the EU Early Warning System [2]. The continued emergence of synthetic cannabinoids in the recreational and illicit drug markets has caused unforeseen consequences and has become a global public health problem [3,4,5,6,7,8,9]. AM-2201 (Figure 1) is a third-generation synthetic cannabinoid modified by introducing a fluorine atom into the JGH compound, exerting potent pharmacological effects on brain function and causing psychoactive and addictive effects [Ten].
Molecules 22 00443 g001 550 Figure 1. Chemical structure of AM-2201, AM 2201 chemical for sale
It is increasingly found in recreational users and cases of poisoning, and in herbal products marketed for recreational use. B. Incense blends [3,6,7,11,12,13,14,15,16,17,18]. The enzymes cytochrome P450 (CYP) 1A2 and CYP2C9 play key roles in the metabolism of AM-2201 to 4-hydroxyfluoropentyl-AM-2201, AM-2201-pentanoic acid, and 5-hydroxypentyl-AM-2201. Buy AM 2201 online, AM 2201 drug, AM 2201 for sale, AM 2201 chemical, where to buy AM 2201
Variability of drug metabolism due to inhibition and induction of uridine 5′-diphospho-glucuronosyltransferase (UGT) enzymes, as well as CYP enzymes, is an important complicating factor in pharmacology and toxicology, drug therapy, environmental exposure, and risk assessment .
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Phytocannabinoids, such as THC, cannabidiol, and cannabinol, inhibit CYPs 1A1, 1A2, 2A6, 2B6, 2C9, 2D6, 3A4, and 3A5 activities in human liver microsomes and recombinant CYP enzymes; cannabidiol is the most potent inhibitor of many CYPs [22,23,24,25,26,27,28,29].
Cannabidiol inhibited UGT1A9 and UGT2B7 activities, and cannabinol inhibited UGT1A9 activity in human liver and intestine microsomes and recombinant UGT enzymes [30]. Understanding the roles of synthetic cannabinoids in the regulation of CYP and UGT is necessary to predict individual differences in synthetic cannabinoid toxicity and to prevent toxic drug–drug interactions; however, the effects of synthetic cannabinoids, including AM-2201, on the regulation of CYP and UGT enzymes remain largely unknown.
In this study, the inhibitory effects of AM-2201 on eight major human CYP activities (CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4) and six major UGT activities (UGTs 1A1, 1A3, 1A4, 1A6, 1A9, and 2B7) were examined using pooled human liver microsomes to evaluate the possibility of AM-2201-induced drug interactions.
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