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MAM-2201
MAM-2201 (4'-methyl-AM-2201, 5"-fluoro-JWH-122) is a drug that presumably acts as a potent agonist for the cannabinoid receptors. It had never previously been reported in the scientific or patent literature, and was first identified by laboratories in the Netherlands and Germany in June 2011 as an ingredient in synthetic cannabis smoking blends. Like RCS-4 and AB-001, MAM-2201 thus appears to be a novel compound invented by " research chemical" suppliers specifically for grey-market recreational use. Structurally, MAM-2201 is a hybrid of two known cannabinoid compounds JWH-122 and AM-2201, both of which had previously been used as active ingredients in synthetic cannabis blends before being banned in many countries. A study of MAM-2201 in rats showed that it causes neurofunctional disruptions. Legal status In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as MAM-2201 are Schedule I Controlled Substances. MAM-2201 has been banned by being ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Scheduling Of Synthetic Cannabinoids
To combat the illicit synthetic cannabinoid industry many jurisdictions have created a system to control these cannabinoids through their general (or Markush) structure as opposed to their specific identity. In this way new analogs are already controlled before they are even created. A large number of cannabinoids have been grouped into classes based on similarities in their chemical structure, and these classes have been widely adopted across a variety of jurisdictions. Typical groups of compounds included for control may include naphthoylindoles, phenylacetylindoles, benzoylindoles, cyclohexylphenols, naphthylmethylindoles, naphthoylpyrroles, naphthylmethylindenes, indole-3-carboxamides, indole-3-carboxylates, indazole-3-carboxamides and sometimes others, each with specific substitutions on specific atoms of the molecule. The scope of definitions and the range of compounds included may vary substantially between jurisdictions, so compounds which are legal in one country or state m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Temporary Class Drug
A temporary class drug is a relatively new status for controlled drugs, which has been adopted in some jurisdictions, notably New Zealand and the United Kingdom, to attempt to bring newly synthesised designer drugs under legal control. The controlled drug legislation in these jurisdictions requires drug scheduling decisions to follow an evidence-based process, where the harms of the drug are assessed and reviewed so that an appropriate legal status can be assigned. Since many designer drugs sold in recent years have had little or no published research that could help inform such a decision, they have been widely sold as "legal highs", often for months, before sufficient evidence accumulates to justify placing them on the controlled drug schedules. This situation has been deemed to be undesirable, as every time a designer drug has been banned, novel compounds with similar effects have been quickly developed and brought to market, often with worse health consequences reported than th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5F-JWH-398
5F-JWH-398 (4'-chloro-AM-2201, Cl-2201, CLAM, SGT-20) is a recreational designer drug which is classed as a synthetic cannabinoid. It is from the naphthoylindole family, and produces cannabis-like effects. It was legally sold in New Zealand from 2012-2014 under the psychoactive substances scheme but was discontinued in May 2014 following the end of the interim approval period under the Psychoactive Substances Act 2013. Subsequently it has appeared on the illicit market around the world and was identified in Germany in May 2019. See also * AM-2201 * JWH-398 * MAM-2201 MAM-2201 (4'-methyl-AM-2201, 5"-fluoro-JWH-122) is a drug that presumably acts as a potent agonist for the cannabinoid receptors. It had never previously been reported in the scientific or patent literature, and was first identified by laborato ... References Naphthoylindoles Organofluorides Designer drugs CB1 receptor agonists CB2 receptor agonists Chloroarenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AM-2201
AM-2201 (1-(5-fluoropentyl)-3-(1-naphthoyl)indole) is a recreational designer drug that acts as a potent but nonselective full agonist for the cannabinoid receptor. It is part of the AM series of cannabinoids discovered by Alexandros Makriyannis at Northeastern University. Hazards Convulsions have been reported including at doses as low as 10 mg. Pharmacology AM-2201 is a full agonist for cannabinoid receptors. Affinities are: with a ''K''i of 1.0 nM at CB1 and 2.6 nM at CB2. The 4-methyl functional analog MAM-2201 probably has similar affinities. AM-2201 has an EC50 of 38 nM for human CB1 receptors, and 58 nM for human CB2 receptors. AM-2201 produces bradycardia and hypothermia in rats at doses of 0.3–3 mg/kg, comparable to the potency of JWH-018 in rats, suggesting potent cannabinoid-like activity. Pharmacokinetics AM-2201 metabolism differs only slightly from that of JWH-018. AM-2201 ''N''- dealkylation produces fluoropentane instead ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NM-2201
NM-2201 (also known as CBL-2201) is an indole-based synthetic cannabinoid that presumably has similar properties to the closely related 5F-PB-22 and NNE1, which are both full agonists and unselectively bind to CB1 and CB2 receptors with low nanomolar affinity. Pharmacology NM-2201 acts as a full agonist with a binding affinity of 0.332 nM at CB1 and 0.732 nM at CB2 cannabinoid receptors. It has been linked to serious adverse events in users. Legal status NM-2201 is specifically banned in Sweden, Germany (Anlage II), and Japan but is also controlled in many other jurisdictions under analogue laws. On May 30, 2018 the United States Drug Enforcement Administration, Department of Justice published a notice of intent to place NM-2201 and 4 other synthetic cannabinoids in schedule I of the Controlled Substances Act. This notice went into effect on June 29, 2018. Use NM-2201 was linked to an incident in December 2015 where 25-30 people in Ocala, FL were taken to h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EAM-2201
EAM-2201 (4'-ethyl-AM-2201, 5"-fluoro-JWH-210, SGT-14) is a drug that presumably acts as a potent agonist for the cannabinoid receptors. It had never previously been reported in the scientific or patent literature, and was first identified by laboratories in Japan in July 2012 as an ingredient in synthetic cannabis smoking blends Like the closely related MAM-2201 which had been first reported around a year earlier, EAM-2201 thus appears to be another novel compound invented by designer drug suppliers specifically for recreational use. Structurally, EAM-2201 is a hybrid of two known cannabinoid compounds JWH-210 and AM-2201, both of which had previously been used as active ingredients in synthetic cannabis blends before being banned in many countries. Pharmacology EAM-2201 acts as a full agonist with a binding affinity of 0.380 nM at CB1 and 0.371 nM at CB2 cannabinoid receptors. Legal status In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Organofluorides
Organofluorine chemistry describes the chemistry of the organofluorines, organic compounds that contain the carbon–fluorine bond. Organofluorine compounds find diverse applications ranging from oil and water repellents to pharmaceuticals, refrigerants, and reagents in catalysis. In addition to these applications, some organofluorine compounds are pollutants because of their contributions to ozone depletion, global warming, bioaccumulation, and toxicity. The area of organofluorine chemistry often requires special techniques associated with the handling of fluorinating agents. The carbon–fluorine bond Fluorine has several distinctive differences from all other substituents encountered in organic molecules. As a result, the physical and chemical properties of organofluorines can be distinctive in comparison to other organohalogens. # The carbon–fluorine bond is one of the strongest in organic chemistry (an average bond energy around 480 kJ/molKirsch, Peer ''Modern fluoroor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects, and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human trials, the use of some of these drugs may result ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
THJ-2201
THJ-2201 is an indazole-based synthetic cannabinoid that presumably acts as a potent agonist of the CB1 receptor and has been sold online as a designer drug. It is a structural analog of AM-2201 in which the central indole ring has been replaced by indazole. Pharmacology THJ-2201 acts as a full agonist with a binding affinity of 1.34nM at CB1 and 1.32nM at CB2 cannabinoid receptors. Side effects THJ-2201 has been linked to at least one hospitalization and death due to its use. Legal status Because of the hazards associated with recreational use of this compound, it is classified as a Schedule I controlled substance in the United States. It is also an Anlage II controlled drug in Germany. See also * AM-694 * AM-1235 * AM-2232 * AM-2233 * FUBIMINA * JWH-018 * List of AM cannabinoids Alexandros Makriyannis is a professor in the Department of Medicinal Chemistry at Northeastern University, where his research group has synthesized many new compounds with cannabi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor
Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids; plant cannabinoids (such as Tetrahydrocannabinol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and phytocannabinoids (plant based cannabinoids) are lipophilic. There are two known subtypes of cannabinoid receptors, termed CB1 and CB2. The CB1 receptor is expressed mainly in the brain (central nervous system or "CNS"), but also in the lungs, liver and kidneys. The CB2 receptor is expressed mainly in the immune system, in hematopoietic cells, and in parts of the brain. The protein sequences of CB1 and CB2 receptors are about 44% simi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
