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5F-APINACA
5F-APINACA (also known as 5F-AKB-48 or 5F-AKB48) is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. Structurally it closely resembles cannabinoid compounds from patent WO 2003/035005 but with a 5-fluoropentyl chain on the indazole 1-position, and 5F-APINACA falls within the claims of this patent, as despite not being disclosed as an example, it is very similar to the corresponding pentanenitrile and 4-chlorobutyl compounds which are claimed as examples 3 and 4. 5F-APINACA was first identified in South Korea. It is expected to be a potent agonist of the CB1 receptor and CB2 receptor. Its metabolism has been described in literature. Pharmacology 5F-APINACA acts as a full agonist with a binding affinity of 1.94 nM at CB1 and 0.266 nM at CB2 cannabinoid receptors. Legality In the United States, 5F-APINACA is a Schedule I controlled substance This is the list of Schedule I drugs as defined by the United States Controlled Sub ...
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5F-AMB
5F-AMB (also known as 5F-MMB-PINACA and 5F-AMB-PINACA) is an indazole-based synthetic cannabinoid from the indazole-3-carboxamide family, which has been used as an active ingredient in synthetic cannabis products. It was first identified in Japan in early 2014. Although only very little pharmacological information about 5F-AMB itself exists, its 4-cyanobutyl analogue (instead of 5-fluoropentyl) has been reported to be a potent agonist for the CB1 receptor (''K''I = 0.7 nM). Side effects 5F-AMB intoxication caused one fatality on its own, another through ketoacidosis in combination with AB-CHMINACA, AB-FUBINACA, AM-2201, 5F-APINACA, EAM-2201, JWH-018, JWH-122, MAM-2201, STS-135 and THJ-2201 and another fatality in combination with AB-CHMINACA and Diphenidine. Legality In the United States, 5F-AMB is a Schedule I controlled substance. 5F-AMB is an Anlage II controlled substance in Germany as of May 2015. Sweden's public health agency suggested classify ...
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ADB-FUBINACA
ADB-FUBINACA is a designer drug identified in synthetic cannabis blends in Japan in 2013. In 2018, it was the third-most common synthetic cannabinoid identified in drugs seized by the Drug Enforcement Administration. The (''S'')-enantiomer of ADB-FUBINACA is described in a 2009 Pfizer patent and has been reported to be a potent agonist of the CB1 receptor and the CB2 receptor with EC50 values of 1.2 nM and 3.5 nM, respectively. ADB-FUBINACA features a carboxamide group at the 3-indazole position, like SDB-001 and STS-135. ADB-FUBINACA appears to be the product of rational drug design, since it differs from AB-FUBINACA only by the replacement of the isopropyl group with a ''tert''-butyl group. An analogue of ADB-FUBINACA, ADSB-FUB-187, containing a more functionalized carboxamide substituent was recently reported. Side effects One death through coronary arterial thrombosis has been linked to ADB-FUBINACA intoxication. At least an additional 8 deaths in Hung ...
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5F-ADB
5F-ADB (also known as 5F-MDMB-PINACA) is an indazole-based synthetic cannabinoid from the indazole-3-carboxamide family, which has been used as an active ingredient in synthetic cannabis products and has been sold online as a designer drug. 5F-ADB is a potent agonist of the CB1 receptor, though it is unclear whether it is selective for this target. 5F-ADB was first identified in November 2014 from post-mortem samples taken from an individual who had died after using a product containing this substance. Subsequent testing identified 5F-ADB to have been present in a total of ten people who had died from unexplained drug overdoses in Japan between September 2014 and December 2014. 5F-ADB is believed to be extremely potent based on the very low levels detected in tissue samples, and appears to be significantly more toxic than earlier synthetic cannabinoid drugs that had previously been sold. In 2018, 5F-ADB was the most common synthetic cannabinoid to be identified in Drug Enforcem ...
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Drugs Controlled By The German Betäubungsmittelgesetz
Drugs controlled by the German ''Betäubungsmittelgesetz'' (BtMG). Trade and 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 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, stereoisomers and salts of the substances listed in ''Anlage I''. '' Anlage II'' ''Anlage II'' controlled substances are tradable, given special permission of the authorities, however not 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''. ''Anlage III'' ''Anlage III'' controlled substances are tradable and prescrip ...
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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 ag ...
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MDMB-CHMICA
MDMB-CHMICA is an indole-based synthetic cannabinoid that is a potent agonist of the CB1 receptor and has been sold online as a designer drug. While MDMB-CHMICA was initially sold under the name "MMB-CHMINACA", the compound corresponding to this code name (i.e. the isopropyl instead of t-butyl analogue of MDMB-CHMINACA) has been identified on the designer drug market in 2015 as AMB-CHMINACA. Chemistry Several commercial samples of MDMB-CHMICA were found to exclusively contain the (''S'')-enantiomer based on vibrational and electronic circular dichroism spectroscopy and X-ray crystallography. An (S)-configuration for the ''tert''-leucinate group is unsurprising since MDMB-CHMICA is likely synthesized from the abundant and inexpensive "L" form of the appropriate ''tert''-leucinate reactant. Pharmacology MDMB-CHMICA acts as a highly potent full agonist of the CB1 receptor with an efficacy of 94% and an EC50 value of 0.14 nM, which is approximately 8 times lower than the ...
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FUB-APINACA
FUB-APINACA (also known as AFUBINACA and FUB-AKB48) is an indazole-based synthetic cannabinoid that is presumed to be a potent agonist of the CB1 receptor and has been sold online as a designer drug. It is an analog of APINACA and 5F-APINACA where the pentyl chain has been replaced with fluorobenzyl. Pharmacology FUB-APINACA acts as a full agonist with a binding affinity of 1.06 nM at CB1 and 0.174 nM at CB2 cannabinoid receptors. Legal status In the United States, FUB-APINACA was temporarily emergency scheduled by the DEA in 2019. and made a permanent Schedule I Controlled Substance nationwide on April 7, 2022. Previously, it was illegal only in Alabama (listed as FUB-AKB48). Sweden's public health agency suggested classifying FUB-APINACA as a hazardous substance on November 10, 2014. See also * 5F-ADB * 5F-AMB * AB-FUBINACA * AB-CHFUPYCA * AB-PINACA * ADAMANTYL-THPINACA * ADB-CHMINACA * ADB-FUBINACA * ADB-PINACA * ADBICA * APP-FUBINACA * FAB-144 * MDMB-CH ...
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APINACA
APINACA (AKB48, ''N''-(1-adamantyl)-1-pentyl-1''H''-indazole-3-carboxamide) is a drug that acts as a reasonably potent agonist for the cannabinoid receptors, with a Ki of 304.5nM and an EC50 of 585nM at CB1. It had never previously been reported in the scientific or patent literature, and was first identified by laboratories in Japan in March 2012 as an ingredient in synthetic cannabis smoking blends, along with a related compound APICA. Structurally, it closely resembles cannabinoid compounds from a University of Connecticut patent (WO 2003/035005), but with a simple pentyl chain on the indazole 1-position, and APINACA falls within the claims of this patent despite not being disclosed as an example. Legality APINACA was made illegal in Japan in 2012, and was banned as a temporary class drug in New Zealand from 13 July 2012. APINACA has been banned in Latvia since 14 November 2013. Since 2013, APINACA has been a Schedule I controlled substance in the United States. It is a ...
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AB-FUBINACA
AB-FUBINACA is a drug that acts as a potent agonist for the cannabinoid receptors, with ''K''i values of 0.9 nM at CB1 and 23.2 nM at CB2 and EC50 values of 1.8 nM at CB1 and 3.2 nM at CB2. It was originally developed by Pfizer in 2009 as an analgesic medication but was never pursued for human use. In 2012, it was discovered as an ingredient in synthetic cannabinoid blends in Japan, along with a related compound AB-PINACA, which had not previously been reported. Its use has been linked to hospitalizations and deaths. Legality It was designated as a Schedule I controlled substance in the United States in January 2014. It is an Anlage II controlled substance in Germany as of November 2014. Since October 2015 AB-FUBINACA is a controlled substance in China . In December 2019, the UNODC announced scheduling recommendations placing AB-FUBINACA as a controlled research chemical into Schedule II. 101789 Mass overdoses due to adulterated K2 On August 15t ...
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ADBICA
ADBICA (also known as ADB-PICA) is a designer drug identified in synthetic cannabis blends in Japan in 2013. ADBICA had not previously been reported in the scientific literature prior to its sale as a component of synthetic cannabis blends. ADBICA features a carboxamide group at the 3-indole position, like SDB-001 and STS-135. The stereochemistry of the tert-butyl side-chain in the product is unresolved, though in a large series of indazole derivatives structurally similar to ADBICA that are disclosed in Pfizer patent WO 2009/106980, activity resides exclusively in the (S) enantiomers. ADBICA is a potent agonist of the CB1 receptor and CB2 receptor with an EC50 value of 0.69 nM and 1.8 nM respectively. Legal Status As of October 2015 ADBICA is a controlled substance in China. See also * 5F-AB-PINACA * 5F-ADB * 5F-ADBICA * 5F-AMB * 5F-APINACA * AB-FUBINACA * AB-CHFUPYCA * AB-CHMINACA * AB-PINACA * ADB-CHMINACA * ADB-FUBINACA * ADB-PINACA * ADB-P7AICA * APICA * APINAC ...
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ADB-PINACA
ADB-PINACA is a cannabinoid designer drug that is an ingredient in some synthetic cannabis products. It is a potent agonist of the CB1 receptor and CB2 receptor with EC50 values of 0.52 nM and 0.88 nM respectively. Like MDMB-FUBINACA, this compound contains an amino acid residue of tert-leucine. Side effects ADB-PINACA has been linked to multiple hospitalizations and deaths due to its use. Metabolism Nineteen ADB-PINACA major metabolites were identified in several incubations with cryopreserved human hepatocytes. Major metabolic reactions included pentyl hydroxylation, hydroxylation followed by oxidation (ketone formation), and glucuronidation. Legality ADB-PINACA is listed in the Fifth Schedule of the Misuse of Drugs Act (MDA) and therefore illegal in Singapore as of May 2015. In the United States, it is a Schedule I controlled substance. As of October 2015 ADB-PINACA is a controlled substance in China. See also * 5F-AB-PINACA * 5F-ADB * 5F-ADB-PINACA ...
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PX-3
PX-3 (also known as APP-CHMINACA) is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor with a binding affinity of ''K''i = 47.6 nM and was originally developed by Pfizer in 2009 as an analgesic An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ... medication. The acronym 'APP' signifies the 'amino', 'phenyl' and 'propanone' elements of the structure. Three related compounds, PX-1 (5F-APP-PICA, SRF-30), PX-2 (5F-APP-PINACA, FU-PX) and APP-FUBINACA were reported by the EMCDDA in late 2014. Legality Sweden's public health agency suggested to classify APP-CHMINACA as hazardous substance on June 1, 2015. See also * 5F-AB-PINACA * 5F-ADB * 5F-AMB * 5F-APINACA * AB-FUBINACA * AB-CHFUPYCA * AB-CHMINACA * AB-PINACA * ADB-CHMI ...
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