SDB-005
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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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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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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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QUCHIC
QUCHIC (BB-22, SGT-32 or 1-(cyclohexylmethyl)-1''H''-indole-3-carboxylic acid 8-quinolinyl ester) is a designer drug offered by online vendors as a cannabimimetic agent, and was first detected being sold in synthetic cannabis products in Japan in early 2013, and subsequently also in New Zealand. The structure of QUCHIC appears to use an understanding of structure-activity relationships within the indole class of cannabimimetics, although its design origins are unclear. QUCHIC, along with QUPIC, represents a structurally unique synthetic cannabinoid chemotype since it contains an ester linker at the indole 3-position rather than the precedented ketone of JWH-018 and its analogues, or the amide of SDB-001 and its analogues. Pharmacology BB-22 acts as a full agonist with a binding affinity of 0.217nM at CB1 and 0.338nM at CB2 cannabinoid receptors. See also * 5F-PB-22 * JWH-018 * PB-22 * QUPIC * SDB-001 * SDB-005 SDB-005 is an indazole-based synthetic cannabinoid that has b ...
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SDB-006
SDB-006 is a drug that acts as a potent agonist for the cannabinoid receptors, with an EC50 of 19 nM for human CB2 receptors, and 134 nM for human CB1 receptors. It was discovered during research into the related compound SDB-001 which had been sold illicitly as "2NE1". SDB-006 metabolism has been described in literature. See also * 5F-CUMYL-PINACA * 5F-SDB-006 * APINACA * CUMYL-PICA * CUMYL-PINACA * CUMYL-THPINACA * SDB-001 * SDB-005 * STS-135 STS-135 ( ISS assembly flight ULF7) was the 135th and final mission of the American Space Shuttle program. It used the orbiter ''Atlantis'' and hardware originally processed for the STS-335 contingency mission, which was not flown. STS-135 la ... References Cannabinoids Designer drugs Indoles Indolecarboxamides {{cannabinoid-stub ...
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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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5F-PB-22
5F-PB-22 (5F-QUPIC or quinolin-8-yl 1-pentyfluoro-1''H''-indole-3-8-carboxylate) is a designer drug which acts as a cannabinoid agonist. The structure of 5F-PB-22 appears to have been designed with an understanding of structure–activity relationships within the indole class of cannabinoids. Pharmacology 5F-PB-22 acts as a full agonist with a binding affinity of 0.468 nM at CB1 and 0.633 nM at CB2 cannabinoid receptors. Legal status As of October 2015 5F-PB-22 is a controlled substance in China. In January 2014, 5F-PB-22 was designated as a Schedule I controlled substance in the United States after several deaths were associated with its use. In the United Kingdom, 5F-PB-22 is now classified and controlled as a Class B drug, following the November 2016 amendment to the Misuse of Drugs Act 1971. Several other synthetic cannabinoids structurally related to JWH-018, like 5F-PB-22, were also classified in this amendment. See also * AM-2201 * JWH-018 * QUCHIC * QU ...
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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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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- ...
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EMCDDA
The European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) is an agency of the European Union located in Lisbon, Portugal, and established in 1993. In June 2022, the Council of the European Union approved a reform of the organization which will lead to an extension of its mandate and a change of name for "European Union Drugs Agency." The EMCDDA strives to be the "reference point" on drug usage for the European Union's member states, and to deliver "factual, objective, reliable and comparable information" about drug usage, drug addiction and related health complications, including hepatitis, HIV/AIDS and tuberculosis. Though the EMCDDA primarily serves Europe, it also works with other partners, scientists and policy-makers around the world. Mission and role The EMCDDA was founded on the principle that independent scientific research is a "vital resource to help Europe understand the nature of its drug problems and better respond to them." Its stated missions are to: ...
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Indazoles
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole. Indazole is an Amphoterism, 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 ; i ...
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CB2 Receptor
The cannabinoid receptor type 2, abbreviated as CB2, is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the ''CNR2'' gene. It is closely related to the cannabinoid receptor type 1 (CB1), which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol (THC), the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). The principal endogenous ligand for the CB2 receptor is 2-Arachidonoylglycerol (2-AG). CB2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol. The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor type 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of ca ...
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