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AM-1220
AM-1220 is a drug that acts as a potent and moderately selective agonist for the cannabinoid receptor CB1, with around 19 times selectivity for CB1 over the related CB2 receptor. It was originally invented in the early 1990s by a team led by Thomas D'Ambra at Sterling Winthrop, but has subsequently been researched by many others, most notably the team led by Alexandros Makriyannis at the University of Connecticut. The (piperidin-2-yl)methyl side chain of AM-1220 contains a stereocenter, so there are two enantiomers with quite different potency, the (''R'')-enantiomer having a Ki of 0.27 nM at CB1 while the (''S'')-enantiomer has a much weaker Ki of 217 nM. Related compounds A number of related compounds are known with similar potent cannabinoid activity, with modifications such as substitution of the indole ring at the 2- or 6-positions, the naphthoyl ring substituted at the 4-position or replaced by substituted benzoyl rings or other groups, or the 1-(N-methylpiperi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AM Cannabinoids
Alexandros Makriyannis is a professor in the Department of Medicinal Chemistry at Northeastern University, where his research group has synthesized many new compounds with cannabinoid activity. Some of those are: See also * List of CP cannabinoids * List of JWH cannabinoids * List of HU cannabinoids A research group led by Raphael Mechoulam at Hebrew University has synthesized many cannabinoids. Some of those are: * HU-210 — a high affinity CB1 agonist (''K''i = 0.23 nM) * HU-211 — the (+)-enantiomer of HU-210 with dramatically re ... * List of miscellaneous designer cannabinoids References {{Cannabinoids ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabipiperidiethanone
Cannabipiperidiethanone (CPE or 1-(N-methylpiperidin-2-ylmethyl)-3-(2-methoxyphenylacetyl)indole) is a synthetic cannabinoid that has been found as an ingredient of "herbal" synthetic cannabis blends sold in Japan, alongside JWH-122 and JWH-081. Its binding affinity was measured at the CB1 and CB2 receptors and it was found to have an IC50 of 591 nM at CB1 and 968 nM at CB2, making it 2.3 times and 9.4 times weaker than JWH-250 at these two targets respectively. In the United States, CB1 receptor agonists of the 3-phenylacetylindole class such as cannabipiperidiethanone are Schedule I Controlled Substances. See also * AM-1220 * AM-1248 * AM-2233 * 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 a ... * RCS-8 References External linksWater Soluble CBD Oil< ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AM-2233
AM-2233 is a drug that acts as a highly potent full agonist for the cannabinoid receptors, with a ''K''i of 1.8 nM at CB1 and 2.2 nM at CB2 as the active (''R'') enantiomer. It was developed as a selective radioligand for the cannabinoid receptors and has been used as its 131I derivative for mapping the distribution of the CB1 receptor in the brain. AM-2233 was found to fully substitute for THC in rats, with a potency lower than that of JWH-018 but higher than WIN 55,212-2. It is notable for inducing tinnitus, though the reasons for this are unclear and may provide valuable insight into tinnitus research. Legal Status As of October 2015 AM-2233 is a controlled substance in China. See also * AM-679 * AM-694 * AM-1220 * AM-1221 * AM-1235 * AM-1241 * AM-2232 * Cannabipiperidiethanone * FUBIMINA * JWH-018 * List of AM cannabinoids * List of JWH cannabinoids * List of HU cannabinoids * List of designer drugs Designer drugs are structural or functional anal ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AM-1248
AM-1248 is a drug that acts as a moderately potent agonist for both the cannabinoid receptors CB1 and CB2, but with some dispute between sources over its exact potency and selectivity. Replacing the 3-(1-naphthoyl) group found in many indole derived cannabinoid ligands, with an adamant oyl group, generally confers significant CB2 selectivity, but reasonable CB1 affinity and selectivity is retained when an N-methylpiperidin-2-ylmethyl substitution is used at the indole 1-position. The related compound 1-pentyl-3-(1-adamantoyl)indole was identified as having been sold as a cannabinoid designer drug in Hungary in 2011, along with another synthetic cannabinoid AM-679. Legality Sweden's public health agency suggested to classify AM-1248 as hazardous substance on June 1, 2015. As of October 2015 AM-1248 is a controlled substance in China. See also * A-834,735 * AB-001 * AM-411 * AM-1220 AM-1220 is a drug that acts as a potent and moderately selective agonist for the cannab ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AM-1221
AM-1221 is a drug that acts as a potent and selective agonist for the cannabinoid receptor CB2, with a ''K''i of 0.28 nM at CB2 and 52.3 nM at the CB1 receptor, giving it around 180 times selectivity for CB2. The 2- methyl and 6- nitro groups on the indole ring both tend to increase CB2 affinity while generally reducing affinity at CB1, explaining the high CB2 selectivity of AM-1221. However, despite this relatively high selectivity for CB2, its CB1 affinity is still too strong to make it useful as a truly selective CB2 agonist, so the related compound AM-1241 is generally preferred for research purposes. In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as AM-1221 are Schedule I Controlled Substances. Legal status It is illegal to supply, trade, sell, distribute, import or transport the pharmaceutical drug in the UK under the Psychoactive Substances Act 2016 which was inforce on May 26th 2016. See also * AM-630 * AM-1220 ... [...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 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)methyl substituent of A-834,735, resulting in compounds that still show significant affinity and efficacy at both receptors despite being CB2 selective overall. Legal status As of October 2015 A-834,735 is a controlled substance in China. See also * ... [...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 Receptors can be activated by either agonists (such as[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychoactive Substances Act 2016
The Psychoactive Substances Act 2016 (c. 2) is an Act of the Parliament of the United Kingdom intended to restrict the production, sale and supply of a new class of psychoactive substances often referred to as "legal highs". The bill was given Royal Assent on 28 January 2016, and came into force on 26 May 2016 across the entire United Kingdom. Description The law defines as a "psychoactive substance" anything which "by stimulating or depressing the person’s central nervous system ... affects the person’s mental functioning or emotional state". The law bans all such substances but exempts alcohol, tobacco or nicotine-based products, caffeine, food and drink, medicinal products and any drug that is already regulated under the Misuse of Drugs Act 1971. The Act: * makes it an offence to produce, supply, offer to supply, possess with intent to supply, possess on custodial premises, import or export psychoactive substances; that is, any substance intended for human cons ... [...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 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Piperidines
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, and typical of amines. The name comes from the genus name '' Piper'', which is the Latin word for pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: : C5H5N + 3 H2 → C5H10NH Pyridine can also be re ... [...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 invented by pharmaceutical company Sterling-Winthrop in the early 1990s as potential nonsteroidal anti-inflammatory agents. 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 Chemical Entities of Biological Interest, also known as ChEBI, is a chemical database and ontology of molecular entities focused on 'small' chemical compounds, that is part of the Open Biomedical Ontologies (OBO) effort at the European Bioinf ... ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naphthoylindoles
Naphthoylindoles are a class of synthetic cannabinoids 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 syntheti .... See also * Structural scheduling of synthetic cannabinoids References {{reflist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
