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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, but did not effect 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 6.9x higher than rat CB1 receptors. Discovery MDA-19 was first synthesized and studied in the late 2000s by researchers at the University of Texas M. D. Anderson Cancer Center. Pharmacology MDA-19 binds to human CB2 receptors at Ki = 43.3 +/- 10.3 nM and human CB1 receptors at Ki = 162.4 +/- 7.6 nM and functions as an agonist in human cannabinoid receptors but functions differently in rat cannabinoid receptors binding to rat canna ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BZO-CHMOXIZID
BZO-CHMOXIZID (CHM-MDA-19) is a synthetic cannabinoid compound first reported in 2008 in the same series as the better known derivative 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 st .... It started to be widely sold as an ingredient in grey-market synthetic cannabis blends in 2021 following the introduction of legislation in China which for the first time introduced general controls on various classes of synthetic cannabinoids, but did not include the group to which MDA-19 and BZO-CHMOXIZID belong. While BZO-CHMOXIZID is the most potent compound at CB1 from this so-called "OXAZID" series, it is still markedly CB2 selective and of relatively low potency at CB1, with an EC50 of 84.6 nM at CB1 compared to 2.21 nM at CB2. References Cannabinoids Hydrazides Cyclohexyl ... [...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. See also * A-834,735 * JTE-907 * MDA-19 * N-(S)-Fenchyl-1-(2-morpholinoethyl)-7-methoxyindole-3-carboxamide * S-444,823 * XLR-12 XLR-12 is an indole-based synthetic cannabinoid drug that was invented by Abbott Laboratories in 2006. It is an analogue of XLR-11 where the 5-fluoropentyl chain has been replaced with a 4,4,4-trifluorobutyl chain. XLR-12 is relatively highly s ... References External links Cannabinoids Japan Tobacco {{cannabinoid-stub ... [...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] |
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% simila ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor 2
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropathic Pain
Neuropathic pain is pain caused by damage or disease affecting the somatosensory system. Neuropathic pain may be associated with abnormal sensations called dysesthesia or pain from normally non-painful stimuli ( allodynia). It may have continuous and/or episodic ( paroxysmal) components. The latter resemble stabbings or electric shocks. Common qualities include burning or coldness, "pins and needles" sensations, numbness and itching. Up to 7%-8% of the European population is affected, and in 5% of persons it may be severe. Neuropathic pain may result from disorders of the peripheral nervous system or the central nervous system (brain and spinal cord). Thus, neuropathic pain may be divided into peripheral neuropathic pain, central neuropathic pain, or mixed (peripheral and central) neuropathic pain. Neuropathic pain may occur in isolation or in combination with other forms of pain. Medical treatments focus on identifying the underlying cause and relieving pain. In cases of neurop ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JWH-007
JWH-007 is an analgesic chemical from the naphthoylindole family, which acts as a cannabinoid agonist at both the CB1 and CB2 receptors. It was first reported in 1994 by a group including the noted cannabinoid chemist John W. Huffman. It was the most active of the first group of ''N''-alkyl naphoylindoles discovered by the team led by John W Huffman, several years after the family was initially described with the discovery of the ''N''-morpholinylethyl compounds pravadoline (WIN 48,098), JWH-200 (WIN 55,225) and WIN 55,212-2 by the Sterling Winthrop group. Several other ''N''-alkyl substituents were found to be active by Huffman's team including the ''n''-butyl, ''n''- hexyl, 2- heptyl, and cyclohexyl ethyl groups, but it was subsequently determined that the 2-methyl group on the indole ring is not required for CB1 binding, and tends to increase affinity for CB2 instead. Consequently, the 2-desmethyl derivative of JWH-007, JWH-018, has slightly higher binding affinity for C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JWH-116
JWH-116 is a synthetic cannabinoid receptor ligand from the naphthoylindole family. It is the indole 2-ethyl derivative of related compound JWH-018. The binding affinity of JWH-116 for the CB1 receptor is reported as Ki = 52 ± 5 nM. In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-116 are Schedule I Controlled Substances. See also * JWH-018 * JWH-081 References JWH cannabinoids Naphthoylindoles Designer drugs CB1 receptor agonists {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JWH-196
JWH-196 is a synthetic cannabinoid receptor ligand from the naphthylmethylindole family. It is the indole 2-methyl derivative of related compound JWH-175, and the carbonyl reduced analog of JWH-007. The binding affinity of JWH-196 for the CB1 receptor is reported as Ki = 151 ± 18 nM. In the United States, all CB1 receptor agonists of the 3-(1-naphthylmethane)indole class such as JWH-196 are Schedule I Controlled Substances. See also * JWH-007 JWH-007 is an analgesic chemical from the naphthoylindole family, which acts as a cannabinoid agonist at both the CB1 and CB2 receptors. It was first reported in 1994 by a group including the noted cannabinoid chemist John W. Huffman. It was t ... * JWH-175 References JWH cannabinoids CB1 receptor agonists 1-Naphthyl compounds Indoles {{cannabinoid-stub ... [...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] |
JWH-015
JWH-015 is a chemical from the naphthoylindole family that acts as a subtype-selective cannabinoid agonist. Its affinity for CB2 receptors is 13.8 nM, while its affinity for CB1 is 383 nM, meaning that it binds almost 28 times more strongly to CB2 than to CB1. However, it still displays some CB1 activity, and in some model systems can be very potent and efficacious at activating CB1 receptors, and therefore it is not as selective as newer drugs such as JWH-133. It has been shown to possess immunomodulatory effects, and CB2 agonists may be useful in the treatment of pain and inflammation. It was discovered and named after John W. Huffman. Metabolism JWH-015 has been shown ''in vitro'' to be metabolized primarily by hydroxylation and ''N''-dealkylation, and also by epoxidation of the naphthalene ring, similar to the metabolic pathways seen for other aminoalkylindole cannabinoids such as WIN 55,212-2. Epoxidation of polycyclic aromatic hydrocarbons (see for example benz ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JWH-047
JWH-047 is a selective cannabinoid ligand that binds to both CB1 and CB2. It has a bindining affinity of Ki = 0.9 nM for the CB2 subtype, and more than 65 times selectivity over the CB1. In the United States, all CB1 receptor agonists of the 3-(1-naphthoyl)indole class such as JWH-047 are Schedule I Controlled Substances. See also *JWH-015 *JWH-018 * JWH-019 *JWH-073 JWH-073, a synthetic cannabinoid, is an analgesic chemical from the naphthoylindole family that acts as a partial agonist at both the CB1 and CB2 cannabinoid receptors. It is somewhat selective for the CB1 subtype, with affinity at this subtype ap ... References Naphthoylindoles JWH cannabinoids CB1 receptor agonists CB2 receptor agonists {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
