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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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5F-CUMYL-PINACA
5F-CUMYL-PINACA (also known as SGT-25 and sometimes sold in e-cigarette form as C-Liquid) is an indazole-3-carboxamide based synthetic cannabinoid. 5F-CUMYL-PINACA acts as a potent agonist for the cannabinoid receptors, with the original patent claiming approximately 4x selectivity for CB1, having an EC50 of <0.1 nM for human CB1 receptors and 0.37 nM for human CB2 receptors. In more recent assays using different techniques, 5F-CUMYL-PINACA was variously found to have an EC50 of 0.43 nM at CB1 and 11.3 nM at CB2, suggesting a somewhat higher CB1 selectivity of 26 times, or alternatively 15.1 nM at CB1 and 34.8 nM at CB2 with only 2.3 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CUMYL-PINACA
CUMYL-PINACA (also known as SGT-24) is an indazole-3-carboxamide based synthetic cannabinoid. CUMYL-PINACA acts as a potent agonist for the cannabinoid receptors, with approximately 3x selectivity for CB1, having an EC50 of 0.15nM for human CB1 receptors and 0.41nM for human CB2 receptors. In its pure form, it is described as a sticky oil which can cause poisoning through transdermal exposure. Legal status Sweden's public health agency suggested classifying CUMYL-PINACA as a hazardous substance, on November 10, 2014. See also * 5F-CUMYL-PINACA * 5F-SDB-006 * CUMYL-4CN-BINACA * CUMYL-PICA * CUMYL-THPINACA * SDB-006 * MN-18 * 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& ... References Cannabinoids Designer drugs Indazolecarboxamides {{cannabinoid-stu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CUMYL-THPINACA
CUMYL-THPINACA (also known as SGT-42) is an indazole-3-carboxamide based synthetic cannabinoid. CUMYL-THPINACA acts as a potent agonist for the cannabinoid receptors, with approximately 6x selectivity for CB1, having an EC50 of 0.1nM for human CB1 receptors and 0.59nM for human CB2 receptors. Legal status Sweden's public health agency suggested to classify CUMYL-THPINACA as hazardous substance on November 10, 2014. As of October 2015 CUMYL-THPINACA is a controlled substance in China. See also * 5F-CUMYL-PINACA * 5F-SDB-006 * ADAMANTYL-THPINACA * CUMYL-4CN-BINACA * CUMYL-CBMINACA * CUMYL-PICA * CUMYL-PINACA * 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 and 45.298& ... References Cannabinoids Designer drugs Indazolecarboxamides {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SDB-001
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 |
Cannabinoid Receptor
Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains. Cannabinoid receptors are activated by three major groups of ligands: endocannabinoids; plant cannabinoids (such as Tetrahydrocannabinol, produced by the cannabis plant); and synthetic cannabinoids (such as HU-210). All of the endocannabinoids and phytocannabinoids (plant based cannabinoids) are lipophilic. There are two known subtypes of cannabinoid receptors, termed CB1 and CB2. The CB1 receptor is expressed mainly in the brain (central nervous system or "CNS"), but also in the lungs, liver and kidneys. The CB2 receptor is expressed mainly in the immune system, in hematopoietic cells, and in parts of the brain. The protein sequences of CB1 and CB2 receptors are about 44% similar. When ... [...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] |
STS-135 (drug)
STS-135 (''N''-(adamantan-1-yl)-1-(5-fluoropentyl)-1''H''-indole-3-carboxamide, also called 5F-APICA) is a designer drug offered by online vendors as a cannabimimetic agent. The structure of STS-135 appears to use an understanding of structure-activity relationships within the indole class of cannabimimetics, although its design origins are unclear. STS-135 is the terminally-fluorinated analogue of SDB-001, just as AM-2201 is the terminally-fluorinated analogue of JWH-018, and XLR-11 is the terminally-fluorinated analogue of UR-144. STS-135 acts a potent cannabinoid receptor agonist in vitro, with an EC50 of 51 nM for human CB2 receptors, and 13 nM for human CB1 receptors. STS-135 produces bradycardia and hypothermia in rats at doses of 1–10 mg/kg, suggesting cannabinoid-like activity. Legal status As of October 2015 STS-135 is a controlled substance in China. It is also illegal in the UK. Detection A forensic standard of STS-135 is available, and the compou ... [...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] |
