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APP-FUBINACA
APP-FUBINACA is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. Pharmacological testing showed APP-FUBINACA to have only moderate affinity for the CB1 receptor, with a Ki of 708 nM, while its EC50 was not tested. It contains a phenylalanine amino acid residue in its structure. Legality Sweden's public health agency suggested to classify APP-FUBINACA as hazardous substance on March 24, 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 * APP-BINACA * BMS-F * MDMB-CHMICA * MDMB-FUBINACA * PX-1 * 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 Cannabinoids Designer drugs Ind ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MDMB-FUBINACA
MDMB-FUBINACA (also known as MDMB(N)-Bz-F and FUB-MDMB) is an indazole-based synthetic cannabinoid that is a potent agonist for the cannabinoid receptors, with ''K''i values of 1.14 nM at CB1 and 0.1228 nM at CB2 and EC50 values of 0.2668 nM at CB1 and 0.1411 nM at CB2, and has been sold online as a designer drug. Its benzyl analogue (instead of 4-fluorobenzyl) has been reported to be a potent agonist for the CB1 receptor (''K''i = 0.14 nM, EC50 = 2.42 nM). The structure of MDMB-FUBINACA contains the amino aci3-methylvalineor tert-leucine methyl ester. Side effects There have been a large number of reported cases of deaths and hospitalizations in relation to this synthetic cannabinoid, mainly in Russia and Belarus. MDMB-FUBINACA was first reported in 2014 and quickly gained a reputation as the most deadly synthetic cannabinoid drug sold by 2015. Up to 700 hospitalisations and 25 deaths were initially linked to MDMB-FUBINACA in media and govern ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BMS-F
BMS-F is a chemical from the aminoalkylindole family invented by Bristol-Myers Squibb around 1999, that acts as a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 8 nM at CB2 and 500x selectivity over the related CB1 receptor. It has antiinflammatory effects and inhibits release of TNF-α. See also * A-796,260 * APP-FUBINACA * JWH-200 * MDMB-FUBINACA * MN-25 * Pravadoline * S-777,469 * WIN 55,212-2 WIN 55,212-2 is a chemical described as an aminoalkylindole derivative, which produces effects similar to those of cannabinoids such as tetrahydrocannabinol (THC) but has an entirely different chemical structure. WIN 55,212-2 is a potent canna ... References {{Cannabinoids Aminoalkylindoles Designer drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Indazole
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole. Indazole is an amphoteric molecule which can be protonated to an indazolium cation or deprotonated to an indazolate anion. The corresponding ''pKa'' values are 1.04 for the equilibrium between indazolium cation and indazole and 13.86 for the equilibrium between indazole and indazolate anion. Indazole derivatives display a broad variety of biological activities. Indazoles are rare in nature. The alkaloids nigellicine, nigeglanine, and nigellidine are indazoles. Nigellicine was isolated from the widely distributed plant ''Nigella sativa'' L. (black cumin). Nigeglanine was isolated from extracts of ''Nigella glandulifera''. The Davis–Beirut reaction can generate 2''H''-indazoles. Indazole, C7H6N2, was obtained by E. Fischer (''Ann.'' 1883, 221, p. 280) by heating ortho-hydrazine cinnamic acid, : Some derivatives ; indazole-3- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...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 i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
