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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 15th, ...
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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
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Research Chemical
Research chemicals are chemical substances used by scientists for medical and scientific research purposes. One characteristic of a research chemical is that it is for laboratory research use only; a research chemical is not intended for human or veterinary use. This distinction is required on the labels of research chemicals, and is what exempts them from regulation under parts 100-740 in Title 21 of the Code of Federal Regulations ( 21CFR). Background Pharmacological research chemicals Research chemicals are fundamental in the development of novel pharmacotherapies. Common medical laboratory uses include ''in vivo'' and animal testing to determine therapeutic value, toxicology testing by contract research organization In the life sciences, a contract research organization (CRO) is a company that provides support to the pharmaceutical, biotechnology, and medical device industries in the form of research services outsourced on a contract basis. A CRO may provid ...s to d ...
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AMB-FUBINACA
AMB-FUBINACA (also known as FUB-AMB and MMB-FUBINACA) is an indazole-based synthetic cannabinoid that is a potent agonist for the cannabinoid receptors, with ''K''i values of 10.04 nM at CB1 and 0.786 nM at CB2 and EC50 values of 0.5433 nM at CB1 and 0.1278 nM at CB2, and has been sold online as a designer drug. It was originally developed by Pfizer which described the compound in a patent in 2009, but was later abandoned and never tested on humans. AMB-FUBINACA was the most common synthetic cannabinoid identified in drug seizures by the Drug Enforcement Administration in 2017 and the first half of 2018. Mass casualties On July 12, 2016, the New York City Emergency Medical Services responded to a "mass casualty event" in Brooklyn, New York, where 33 people ranging in age from 25 to 59 years old were adversely affected by the drug. 18 were hospitalized. All of the victims were described by-standers as “zombielike” and the cause was attributed to u ...
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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-PINACA is a cannabinoi ...
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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 Hungar ...
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ADB-CHMINACA
ADB-CHMINACA (also known as MAB-CHMINACA) is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor with a binding affinity of ''K''i = 0.289 nM and was originally developed by Pfizer in 2009 as an analgesic medication. It was identified in cannabinoid blends in Japan in early 2015. Side effects There have been a number of reported cases of deaths and hospitalizations in relation to this synthetic cannabinoid. Legal status In the United States, ADB-CHMINACA is a Schedule I controlled substance. Prior to its listing at the federal level in 2018, Louisiana placed ADB-CHMINACA on its Schedule I list by emergency scheduling in 2014. Sweden's public health agency suggested to classify ADB-CHMINACA as hazardous substance on November 10, 2014. ADB-CHMINACA is listed in the Fifth Schedule of the Misuse of Drugs Act (MDA) and therefore illegal in Singapore as of May 2015. ADB-CHMINACA is illegal in Switzerland as of December 2015. M ...
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AB-CHMINACA
AB-CHMINACA is an indazole-based synthetic cannabinoid. It is a potent agonist of the CB1 receptor (''K''i = 0.78 nM) and CB2 receptor (''K''i = 0.45 nM) and fully substitutes for Δ9-THC in rat discrimination studies, while being 16x more potent. Continuing the trend seen in other cannabinoids of this generation, such as AB-FUBINACA and AB-PINACA, it contains a valine amino acid amide residue as part of its structure, where older cannabinoids contained a naphthyl or adamantane residue. Side effects There have been a number of reported cases of seizures, deaths, and psychotic episodes in relation to this synthetic cannabinoid. Legal status In 2015, AB-CHMINACA became a Schedule I controlled substance in the United States. AB-CHMINACA is an Anlage II controlled substance in Germany as of May 2015. As of October 2015 AB-CHMINACA is a controlled substance in China. AB-CHMINACA is illegal in Switzerland as of December 2015. AB-CHMINACA is ...
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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. 5F-APINACA is an Anlage II controlled drug in Germany since July 2013. As of October 2 ...
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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 classifying 5F-AM ...
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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 Enforcemen ...
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5F-AB-PINACA
5F-AB-PINACA is an indazole-based synthetic cannabinoid that is derived from a series of compounds originally developed by Pfizer in 2009 as an analgesic medication, and has been sold online as a designer drug. 5F-AB-PINACA has been reported to be a potent agonist of the CB1 receptor and CB2 receptor with EC50 values of 0.48 nM and 2.6 nM respectively. Its metabolism has been described in literature. Legality China As of October 2015 5F-AB-PINACA is a controlled substance in China. Germany 5F-AB-PINACA is an Anlage II controlled substance in Germany as of May 2015. Singapore It is also controlled under the Fifth Schedule of the Misuse of Drugs Act (MDA) in Singapore as of May 2015. See also * 5F-ADB * 5F-AMB * 5F-CUMYL-PINACA * AB-FUBINACA * AB-CHFUPYCA * AB-PINACA * ADB-CHMINACA * ADB-FUBINACA * ADB-PINACA * ADBICA * APICA * APINACA * MDMB-CHMICA * PX-3 PX-3 (also known as APP-CHMINACA) is an indazole-based synthetic cannabinoid. It is a potent ag ...
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