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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 It is a structural analog of AM-2201 in which the central indole ring has been replaced by indazole.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 ...
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Synthetic Cannabinoid
Synthetic cannabinoids are a class of designer drug molecules that bind to the same receptors to which cannabinoids ( THC, CBD and many others) in cannabis plants attach. These novel psychoactive substances should not be confused with synthetic phytocannabinoids (THC or CBD obtained by chemical synthesis) or synthetic endocannabinoids from which they are in many aspects distinct. Typically, synthetic cannabinoids are sprayed onto plant matter and are usually smoked, although they have also been ingested as a concentrated liquid form in the US and UK since 2016. They have been marketed as herbal incense, or "herbal smoking blends", and sold under common names like K2, spice, and synthetic marijuana. They are often labeled "not for human consumption" for liability defense. A large and complex variety of synthetic cannabinoids are designed in an attempt to avoid legal restrictions on cannabis, making synthetic cannabinoids designer drugs. Most synthetic cannabinoids are agon ...
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THJ-018
THJ-018 (SGT-17) is a synthetic cannabinoid that is the indazole analogue of JWH-018 and has been sold online as a designer drug. Pharmacology THJ-018 acts as a full agonist with a binding affinity of 5.84 nM at CB1 and 4.57 nM at CB2 cannabinoid receptors. Legality THJ-018 is an Anlage II controlled drug in Germany. It is also banned in Sweden. See also * THJ-2201 * 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 Makriyanni ... References Cannabinoids Designer drugs Naphthoylindazoles {{cannabinoid-stub ...
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FUBIMINA
FUBIMINA (also known as BIM-2201, BZ-2201 and FTHJ) is a synthetic cannabinoid that is the benzimidazole analog of AM-2201 and has been used as an active ingredient in synthetic cannabis products. It was first identified in Japan in 2013, alongside MEPIRAPIM. FUBIMINA acts as a reasonably potent agonist for the CB2 receptor ( ''K''i = 23.45 nM), with 12x selectivity over CB1 (''K''i = 296.1 nM), and does not fully substitute for Δ9-THC in rat discrimination studies. Related benzimidazole derivatives have been reported to be highly selective agonists for the CB2 receptor. See also * AM-694 * AM-1235 * AM-2232 * AM-2233 * BIM-018 * JWH-018 * List of AM cannabinoids * List of JWH cannabinoids * 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 ha ...
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Drugs Controlled By The German Betäubungsmittelgesetz
Drugs controlled by the German ''Betäubungsmittelgesetz'' (BtMG). Trade and drug possession, possession of these substances without licence or prescription is considered illegal; prescription is illegal for drugs on ''Anlage I'' and II and drugs on ''Anlage III'' require a special prescription form. ''Anlage I'' ''Anlage I'' controlled substances are tradability, non-tradable. Those substances are available only by special permission of the authorities, which is granted only for scientific or other public interest purposes. As well as ester, ether, Stereoisomerism, stereoisomers and salts of the substances listed in ''Anlage I''. '' Anlage II'' ''Anlage II'' controlled substances are tradability, tradable, given special permission of the authorities, however not medical prescription , prescriptible. Narcotics on ''Anlage II'' are usually needed for the production of other narcotics on ''Anlage III''. As well as ester, ether and salts of the substances listed in ''Anlage II'' ...
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JWH-018
JWH-018 (1-pentyl-3-(1-naphthoyl)indole, NA-PIMO or AM-678) is an analgesic chemical from the naphthoylindole family that acts as a full agonist at both the CB1 and CB2 cannabinoid receptors, with some selectivity for CB2. It produces effects in animals similar to those of tetrahydrocannabinol (THC), a cannabinoid naturally present in cannabis, leading to its use in synthetic cannabis products that in some countries are sold legally as "incense blends". As a full agonist at both the CB1 and CB2 cannabinoid receptors, this chemical compound is classified as an analgesic medication. The analgesic effects of cannabinoid ligands, mediated by CB1 receptors are well established in treatment of neuropathic pain, as well as cancer pain and arthritis. These compounds work by mimicking the body's naturally-produced endocannabinoid hormones such as 2-AG and anandamide (AEA), which are biologically active and can exacerbate or inhibit nerve signaling. As the cause is poorly understood in ch ...
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AM-694
AM-694 (1-(5-fluoropentyl)-3-(2-iodobenzoyl)indole) is a designer drug that acts as a potent and selective agonist for the cannabinoid receptor CB1. It is used in scientific research for mapping the distribution of CB1 receptors. Pharmacology AM-694 is an agonist for cannabinoid receptors. It has a ''K''i of 0.08 nM at CB1 and 18 times selectivity over CB2 with a ''K''i of 1.44 nM. It is unclear what is responsible for this unusually high CB1 binding affinity, but it makes the 18F radiolabelled derivative of AM-694 useful for mapping the distribution of CB1 receptors in the body. Metabolism Pathways of metabolism include hydrolytic defluorination, carboxylation, and monohydroxylation of the ''N''-alkyl chain. See also * AM-679 * AM-1235 * AM-2201 * AM-2232 * AM-2233 * FUBIMINA * JWH-018 * List of AM cannabinoids * List of JWH cannabinoids * THJ-2201 THJ-2201 is an indazole-based synthetic cannabinoid that presumably acts as a potent agonist of the C ...
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Schedule I Controlled Substance
This is the list of Schedule I drugs as defined by the United States Controlled Substances Act. 21 CFRbr>1308.11(CSA Sched I) with changes through (Oct 18, 2012). Retrieved September 6, 2013. The following findings are required for drugs to be placed in this schedule: # The drug or other substance has a high potential for abuse. # The drug or other substance has no currently accepted medical use in treatment in the United States. # There is a lack of accepted safety for use of the drug or other substance under medical supervision. Except as specifically authorized, it is illegal for any person: # to manufacture, distribute, or dispense, or possess with intent to manufacture, distribute, or dispense, a controlled substance; or # to create, distribute, dispense, or possess with intent to distribute or dispense, a counterfeit substance. Additional substances are added to the list by the Secretary of Health and Human Services pursuant to 21 CFR 1308.49.
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Cannabinoid
Cannabinoids () are several structural classes of compounds found in the cannabis plant primarily and most animal organisms (although insects lack such receptors) or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary intoxicating compound in cannabis. Cannabidiol (CBD) is a major constituent of temperate Cannabis plants and a minor constituent in tropical varieties. At least 113 distinct phytocannabinoids have been isolated from cannabis, although only four (i.e., THCA, CBDA, CBCA and their common precursor CBGA) have been demonstrated to have a biogenetic origin. It was reported in 2020 that phytocannabinoids can be found in other plants such as rhododendron, licorice and liverwort, and earlier in Echinacea. Phytocannabinoids are multi-ring phenolic compounds structurally related to THC, but endocannabinoids are fatty acid derivatives. Nonclassical synthetic cannabinoids (cannabimimetics) include ami ...
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AM-1235
AM-1235 (1-(5-fluoropentyl)-3-(naphthalen-1-oyl)-6-nitroindole) is a drug that acts as a potent and reasonably selective agonist for the cannabinoid receptor CB1. Pharmacology Pharmacodynamics AM-1235 is a cannabinoid receptor agonist with Ki of 1.5 nM at CB1 compared to 20.4 nM at CB2. While the 6-nitro substitution on the indole ring reduces affinity for both CB1 and CB2 relative to the unsubstituted parent compound AM-2201, CB2 affinity is reduced much more, resulting in a CB1 selectivity of around 13 times. This is in contrast to other related compounds such as AM-1221 where a 6-nitro substitution instead confers significant selectivity for CB2. Pharmacokinetics AM-1235 metabolism differs only slightly from that of JWH-018. AM-1235 ''N''- dealkylation produces fluoropentane instead of pentane (or plain alkanes in general). It has been speculated that the fluoropentane might function as an alkylating agent or is further metabolized into toxic fluoroacetic ...
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AM-2232
AM-2232 (1-(4-cyanobutyl)-3-(naphthalen-1-oyl)indole) is a drug that acts as a potent but unselective agonist for the cannabinoid receptors, with a ''K''i of 0.28 nM at CB1 and 1.48 nM at CB2. In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as AM-2232 are Schedule I Controlled Substances. See also * AM-694 * AM-1235 * AM-2233 * FUBIMINA * JWH-018 * List of AM cannabinoids * List of JWH cannabinoids * O-774 * O-1057 * O-1812 * 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 rep ... References Naphthoylindoles Nitriles AM cannabinoids Designer drugs {{cannabinoid-stub ...
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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 ...
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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 ...
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