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5F-PCN
5F-PCN (also known as 5F-MN-21) is an azaindole-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 closely related to NNE1. 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 5F-PCN may release 1-naphthylamine, a known carcinogen. Legal status Sweden's public health agency suggested to classify 5F-PCN as hazardous substance on November 10, 2014. See also * 5F-NNE1 * AM-2201 * APICA * CUMYL-PICA * CUMYL-5F-P7AICA * JWH-018 * NM-2201 * SDB-005 SDB-005 is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. It is presumed to be an agonist of the CB1 and CB2 cannabinoid receptors. SDB-005 is the indazole core analog of PB-22 where the 8-hydroxyquinoline ... References Designer drugs Naphthoylindoles Indolecarboxamides ...
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NNE1
NNE1 (also known as NNEI, MN-24 and AM-6527) is an indole-based synthetic cannabinoid, representing a molecular hybrid of APICA and JWH-018 that is an agonist for the cannabinoid receptors, with ''K''i values of 60.09 nM at CB1 and 45.298 nM at CB2 and EC50 values of 9.481 nM at CB1 and 1.008 nM at CB2. It was invented by Abbott and has a CB1 receptor pEC50 of 8.9 with around 80x selectivity over the related CB2 receptor. It is suspected that metabolic hydrolysis of the amide group of NNE1 may release 1-naphthylamine, a known carcinogen, given the known metabolic liberation (and presence as an impurity) of amantadine in the related compound APINACA, and NNE1 was banned in New Zealand in 2012 as a temporary class drug to stop it being used as an ingredient in then-legal synthetic cannabis products. NNE1 was subsequently found to be responsible for the death of a man in Japan in 2014. See also * 5F-NNE1 * 5F-PCN * AM-2201 * APICA * CUMYL-PICA * FDU-NNE ...
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CUMYL-5F-P7AICA
5F-CUMYL-P7AICA (also known as CUMYL-5F-P7AICA or SGT-263) is a pyrrolo ,3-byridine-3-carboxamide based synthetic cannabinoid that has been sold as a designer drug. It was first identified by the EMCDDA in February 2015. See also * 5F-A-P7AICA * 5F-AB-P7AICA * 5F-CUMYL-PINACA * 5F-MDMB-P7AICA * 5F-PCN * 5F-SDB-006 * ADB-P7AICA ADB-P7AICA is a cannabinoid designer drug that has been found as an ingredient in some synthetic cannabis products, first identified by the DEA in early 2021. See also * 5F-CUMYL-P7AICA * ADBICA * ADB-PINACA ADB-PINACA is a cannabinoid des ... References Cannabinoids Designer drugs Organofluorides Pyrrolopyridines {{cannabinoid-stub ...
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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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CUMYL-PICA
CUMYL-PICA (SGT-56) is an indole-3-carboxamide based synthetic cannabinoid. It is the α,α-dimethylbenzyl analogue of SDB-006. It was briefly sold in New Zealand during 2013 as an ingredient of at the time legal synthetic cannabis products, but the product containing CUMYL-BICA and CUMYL-PICA was denied an interim licensing approval under the Psychoactive Substances regulatory scheme, due to reports of adverse events in consumers. CUMYL-PICA acts as an agonist for the cannabinoid receptors, with ''K''i values of 59.21 nM at CB1 and 136.38 nM at CB2 and EC50 values of 11.98 nM at CB1 and 16.2 nM at CB2. See also * 5F-CUMYL-PINACA * 5F-SDB-006 * CUMYL-4CN-BINACA * CUMYL-PINACA * CUMYL-THPINACA * SDB-006 * NNE1 NNE1 (also known as NNEI, MN-24 and AM-6527) is an indole-based synthetic cannabinoid, representing a molecular hybrid of APICA and JWH-018 that is an agonist for the cannabinoid receptors, with ''K''i values of 60.09 nM at CB1 an ...
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Naphthoylindoles
Naphthoylindoles are a class of synthetic cannabinoids. See also * Structural scheduling of synthetic cannabinoids To combat the illicit synthetic cannabinoid industry many jurisdictions have created a system to control these cannabinoids through their general (or Markush) structure as opposed to their specific identity. In this way new analogs are already cont ... References {{reflist ...
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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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SDB-005
SDB-005 is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. It is presumed to be an agonist of the CB1 and CB2 cannabinoid receptors. SDB-005 is the indazole core analog of PB-22 where the 8-hydroxyquinoline has also been replaced with a naphthalene group. The code number SDB-005 was originally used for a different compound, the ''N''-phenyl instead of ''N''-benzyl analogue of SDB-006. This compound is a potent agonist of the CB1 receptor (Ki = 21 nM) and CB2 receptor (Ki = 140 nM). However, SDB-005 was subsequently used as the name for the indazole-3-carboxylate compound mentioned above when it was sold in Europe as a designer drug, and was entered into the EMCDDA synthetic drug database under this name. Consequently, there are now two distinct, yet fairly closely related cannabinoid compounds, which may both be referred to under the code SDB-005. See also * 5F-PB-22 * AM-2201 * BB-22 * JWH-018 * NM-2201 * NNE1 NNE1 (also known as N ...
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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 hos ...
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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 chr ...
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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 of p ...
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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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