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PX-1
PX-1 (also known as 5F-APP-PICA and SRF-30) is an indole-based synthetic cannabinoid that has been sold online as a designer drug. Legality Sweden's public health agency suggested classifying PX-1 as hazardous substance on November 10, 2014. PX-1 is listed in the Fifth Schedule of the Misuse of Drugs Act (MDA) and therefore illegal in Singapore as of May 2015. See also * 5F-AB-PINACA * 5F-ADB * 5F-AMB * 5F-APINACA * AB-FUBINACA * AB-CHFUPYCA * AB-CHMINACA * AB-PINACA * ADB-CHMINACA * ADB-FUBINACA * ADB-PINACA * ADBICA * APICA * APINACA * MDMB-CHMICA * PX-2 * 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 m ... References Indoles Cannabinoids Designer drugs Indolecarboxamides Organofluorides {{cannabinoid-stub ...
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PX-2
PX-2 (also known as 5F-APP-PINACA, FU-PX and PPA(N)-2201) is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. It contains a phenylalanine amino acid amide as part of its structure. Legality Sweden's public health agency suggested classifying PX-2 as hazardous substance on November 10, 2014. PX-2 is listed in the Fifth Schedule of the Misuse of Drugs Act (MDA) and therefore illegal in Singapore as of May 2015. As of October 2015 PX-2 is a controlled substance in China. See also * 5F-AB-PINACA * 5F-ADB * 5F-AMB * 5F-APINACA * AB-FUBINACA * AB-CHFUPYCA * AB-CHMINACA * AB-PINACA * ADB-CHMINACA * ADB-FUBINACA * ADB-PINACA * ADBICA * APICA * APINACA * MDMB-CHMICA * PX-1 * 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 m ... References ...
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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 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-CHMINACA * ADB-FUBINACA * ADB-PINACA * ADBICA * APICA * APINACA * MDMB-CHMICA * PX-1 * PX-2 PX-2 (also known as 5F-APP-PINACA, FU-PX and PPA(N)-2201) is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. It contains a phenylala ...
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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 agonists o ...
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Indole
Indole is an aromatic heterocyclic organic compound with the formula C8 H7 N. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indole is widely distributed in the natural environment and can be produced by a variety of bacteria. As an intercellular signal molecule, indole regulates various aspects of bacterial physiology, including spore formation, plasmid stability, resistance to drugs, biofilm formation, and virulence. The amino acid tryptophan is an indole derivative and the precursor of the neurotransmitter serotonin. General properties and occurrence Indole is a solid at room temperature. It occurs naturally in human feces and has an intense fecal odor. At very low concentrations, however, it has a flowery smell, and is a constituent of many perfumes. It also occurs in coal tar. The corresponding substituent is called indolyl. Indole undergoes electrophilic substitution, mainly at position 3 (see diagra ...
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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 i ...
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Cannabinoids
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 amin ...
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Indoles
Indole is an aromatic heterocyclic organic compound with the formula C8 H7 N. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indole is widely distributed in the natural environment and can be produced by a variety of bacteria. As an intercellular signal molecule, indole regulates various aspects of bacterial physiology, including spore formation, plasmid stability, resistance to drugs, biofilm formation, and virulence. The amino acid tryptophan is an indole derivative and the precursor of the neurotransmitter serotonin. General properties and occurrence Indole is a solid at room temperature. It occurs naturally in human feces and has an intense fecal odor. At very low concentrations, however, it has a flowery smell, and is a constituent of many perfumes. It also occurs in coal tar. The corresponding substituent is called indolyl. Indole undergoes electrophilic substitution, mainly at position 3 (see diagram i ...
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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 EC ...
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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 al ...
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APICA (synthetic Cannabinoid Drug)
APICA (2NE1, SDB-001, ''N''-(1-adamantyl)-1-pentyl-1''H''-indole-3-carboxamide) is an indole based drug that 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 March 2012 as an ingredient in synthetic cannabis smoking blends, along with its indazole derivative APINACA (sold as "AKB48"). Structurally it closely resembles cannabinoid compounds from patenWO 2003/035005but with an indole core instead of indazole, and a simple pentyl chain on the indole 1-position. Given the known metabolic liberation (and presence as an impurity) of amantadine in the related compound APINACA, it is suspected that metabolic hydrolysis of the amide group of APICA may also release amantadine. Pharmacological testing determined APICA to have an IC50 of 175 nM at CB1, only slightly less potent than JWH-018 which had an IC50 of 169 nM, but over four times more ...
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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 * APINACA * ...
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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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