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UR-12
MN-25 (UR-12) is a drug invented by Bristol-Myers Squibb, that acts as a reasonably selective agonist of peripheral cannabinoid receptors. It has moderate affinity for CB2 receptors with a ''K''i of 11 nM, but 22x lower affinity for the psychoactive CB1 receptors with a ''K''i of 245 nM. The indole 2-methyl derivative has the ratio of affinities reversed however, with a ''K''i of 8 nM at CB1 and 29 nM at CB2, which contrasts with the usual trend of 2-methyl derivatives having increased selectivity for CB2 (cf. JWH-018 vs JWH-007, JWH-081 vs JWH-098). Chemically, it is closely related to another indole-3-carboxamide synthetic cannabinoid, Org 28611, but with a different cycloalkyl substitution on the carboxamide, and the cyclohexylmethyl group replaced by morpholinylethyl, as in JWH-200 or A-796,260. Early compounds such as these have subsequently led to the development of many related indole-3-carboxamide cannabinoid ligands. See also * A-834,735 * AB- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CUMYL-PEGACLONE
CUMYL-PEGACLONE (SGT-151) is a gamma-carboline based synthetic cannabinoid that has been sold as a designer drug. The gamma-carboline core structure seen in CUMYL-PEGACLONE had not previously been encountered in a designer cannabinoid, though it is similar in structure to other gamma-carboline cannabinoids disclosed by Bristol-Myers Squibb in 2001. Legal status Sweden's public health agency classified CUMYL-PEGACLONE as a narcotic substance, on January 18, 2019. In the United States, the DEA has temporarily placed CUMYL-PEGACLONE into Schedule I status starting on December 12th, 2023 for up to 2 years, during which it's possible the DEA could file for permanent scheduling within those 2 years. If the DEA does not file for permanent placement the temporary Schedule I order will expire on December 12th, 2025. See also * 5F-CUMYL-PEGACLONE * CUMYL-CB-MEGACLONE * CUMYL-CH-MEGACLONE * CUMYL-BC-HPMEGACLONE-221 * CUMYL-PINACA * CUMYL-5F-P7AICA 5F-CUMYL-P7AICA (also known a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bristol-Myers Squibb
The Bristol-Myers Squibb Company, doing business as Bristol Myers Squibb (BMS), is an American multinational pharmaceutical company. Headquartered in Princeton, New Jersey, BMS is one of the world's largest pharmaceutical companies and consistently ranks on the ''Fortune'' 500 list of the largest U.S. corporations. For fiscal 2022, it had a total revenue of $46.2 billion. Bristol Myers Squibb manufactures prescription pharmaceuticals and biologics in several therapeutic areas, including cancer, HIV/AIDS, cardiovascular disease, diabetes, hepatitis, rheumatoid arthritis, and psychiatric disorders. BMS's primary research and development (R&D) sites are located in Lawrence, New Jersey (formerly Squibb, near Princeton), Summit, New Jersey, formerly HQ of Celgene, New Brunswick, New Jersey; Redwood City, California; and Seville in Spain, with other sites in Devens and Cambridge, Massachusetts; Braine-l'Alleud, Belgium; Tokyo, Japan; Hyderabad; Bangalore, India and Wirr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
A-834,735
A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a ''K''i of 12 nM at CB1 and 0.21 nM at CB2. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group of A-834,735 and related compounds imparts significant selectivity for CB2, with most compounds from this group found to be highly selective CB2 agonists with little affinity for CB1. However, low nanomolar CB1 binding affinity In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usuall ... is retained with certain heterocyclic 1-position substituents such as (''N''-methylpiperidin-2-yl)methyl (cf. AM-1220, AM-1248), or the (tetrahydropyran-4-yl)m ... [...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, Australia, and New Zealand, as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these designer drugs 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 tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoids
Cannabinoids () are several structural classes of compounds found primarily in the ''Cannabis'' plant or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary psychoactive compound in cannabis. Cannabidiol (CBD) is also a major constituent of temperate cannabis plants and a minor constituent in tropical varieties. At least 100 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 aminoalkylindoles, 1,5-diarylpyrazoles, quinolines, a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aminoalkylindoles
Aminoalkylindoles (AAIs) are a family of cannabinergic compound that act as a cannabinoid receptor agonist. They were synthesized by the pharmaceutical company Sterling-Winthrop in the early 1990s with a commercial potential as a new family of nonsteroidal anti-inflammatory agents. Aminoalkylindole is a class of synthetic cannabinoid compounds originally developed for cannabinoid receptor pharmacology studies but later emerged as drugs of abuse. They are often found in designer drugs known as synthetic cannabinoids (SCs) or "synthetic marijuana," and their use has been associated with various adverse health effects, including acute kidney injury (AKI) as shown in a 2012 study. Legality Aminoalkylindoles are now commonly found in synthetic cannabis designer drugs. In the United States, the DEA added the aminoalkylindoles JWH-200 to Schedule I of the Controlled Substances Act on 1 March 2011 for 12 months. References {{reflist External links Aminoalkylindoles ChEBI Chemi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
UR-144
UR-144 (TMCP-018, KM-X1, MN-001, YX-17) is a drug invented by Abbott Laboratories, that acts as a selective full agonist of the peripheral cannabinoid receptor CB2, but with much lower affinity for the psychoactive CB1 receptor. Pharmacology UR-144 has high affinity for the CB2 receptor with a Ki of 1.8 nM but 83x lower affinity for the CB1 receptor with a Ki of 150 nM. UR-144 was found to possess an EC50 of 421 nM for human CB1 receptors, and 72 nM for human CB2 receptors. UR-144 produces bradycardia and hypothermia in rats at a dose of 10 mg/kg, suggesting weak cannabinoid-like activity. Chemically it is closely related to other 2,2,3,3-tetramethylcyclopropyl synthetic cannabinoids like A-796,260 and A-834,735 but with a different substitution on the 1-position of the indole core, in these compounds its 1-pentyl group is replaced with alkylheterocycles like 1-(2-morpholinoethyl) and 1-(tetrahydropyran-4-ylmethyl). Legality The UK ACMD recommended that generic prohibit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SR-144,528
SR144528 is a drug that acts as a potent and highly selective CB2 receptor Receptor may refer to: * Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ... inverse agonist, with a Ki of 0.6 nM at CB2 and 400 nM at the related CB1 receptor. It is used in scientific research for investigating the function of the CB2 receptor, as well as for studying the effects of CB1 receptors in isolation, as few CB1 agonists that do not also show significant activity as CB2 agonists are available. It has also been found to be an inhibitor of sterol O-acyltransferase, an effect that appears to be independent from its action on CB2 receptors. See also * NESS-040C5 * Rimonabant * MN-25 References Cannabinoids Chloroarenes Pyrazolecarboxamides {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MDA-19
MDA-19 (also known as BZO-HEXOXIZID) is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB2, with reasonable selectivity over the psychoactive CB1 receptor, though with some variation between species. In animal studies it was effective for the treatment of neuropathic pain Neuropathic pain is pain caused by a lesion or disease of the somatosensory nervous system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli (allodynia). It may have continuo ..., but did not affect rat locomotor activity in that specific study. The pharmacology of MDA-19 in rat cannabinoid receptors have been demonstrated to function differently than human cannabinoid receptors with MDA-19 binding to human CB1 receptors 6.9× higher than rat CB1 receptors. Discovery MDA-19 was first synthesized and studied in the late 2000s by researchers at the University of Texas MD Anderson Cancer Center. Pharm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JWH-203
JWH-203 (1-pentyl-3-(2-chlorophenylacetyl)indole) is an analgesic chemical from the phenylacetylindole family that acts as a cannabinoid agonist with approximately equal affinity at both the CB1 and CB2 receptors, having a Ki of 8.0 nM at CB1 and 7.0 nM at CB2. It was originally discovered by, and named after, John W. Huffman, but has subsequently been sold without his permission as an ingredient of synthetic cannabis smoking blends. Similar to the related 2'-methoxy compound JWH-250, the 2'- bromo compound JWH-249, and the 2'-methyl compound JWH-251, JWH-203 has a phenylacetyl group in place of the naphthoyl ring used in most aminoalkylindole cannabinoid compounds, and has the strongest ''in vitro'' binding affinity for the cannabinoid receptors of any compound in the phenylacetyl group. Unexpectedly despite its weaker CB1 Ki ''in vitro'', the 2-methylindole derivative JWH-204 is actually more potent than JWH-203 in animal tests for cannabinoid activity, thoug ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JTE 7-31
JTE 7-31 is a selective cannabinoid receptor agonist invented by Japan Tobacco. It is a reasonably highly selective CB2 agonist, but still retains appreciable affinity at CB1, with a Ki of 0.088nM at CB2 vs 11nM at CB1. Legality JTE 7-31 is illegal in Alabama Alabama ( ) is a U.S. state, state in the Southeastern United States, Southeastern and Deep South, Deep Southern regions of the United States. It borders Tennessee to the north, Georgia (U.S. state), Georgia to the east, Florida and the Gu .... See also * A-834,735 * JTE-907 * MDA-19 * N-(S)-Fenchyl-1-(2-morpholinoethyl)-7-methoxyindole-3-carboxamide * S-444,823 * XLR-12 References External links Cannabinoids Japan Tobacco {{cannabinoid-stub ... [...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 cannab ... References {{Cannabinoids Aminoalkylindoles Designer drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
