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WIN 54,461
WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2. See also * ADB-5'Br-PINACA * AM-630 (6-Iodopravadoline) * WIN 48,098 (Pravadoline) * WIN 55,212-2 References Cannabinoids Aminoalkylindoles WIN compounds Benzoylindoles 4-Morpholinyl compounds Organobromides {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Inverse Agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; they are in fact sometimes called ''blockers'' (examples include alpha blockers, beta blockers, and calcium channel blockers). Inverse agonists have opposite actions to those of agonists but the effects of both of these can be blocked by antagonists. A prerequisite for an inverse agonist response is that the receptor must have a constitutive (also known as intrinsic or basal) level of activity in the absence of any ligand. An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor
Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system of vertebrates 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; * Phytocannabinoids (plant-derived such as tetrahydrocannabinol (THC) produced by cannabis); * Synthetic cannabinoids (such as HU-210). All endocannabinoids and phytocannabinoids 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 on ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor 2
The cannabinoid receptor 2 (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 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 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the im ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ADB-5'Br-PINACA
ADB-5'Br-PINACA (5'-Br-ADB-PINACA) is an indazole-3-carboxamide based synthetic cannabinoid receptor agonist that has been sold as a designer drug. It was first identified in Abu Dhabi in September 2022 but has subsequently been found in the US and Europe. While formal pharmacology studies have not yet been carried out, ADB-5'Br-PINACA is believed to be a highly potent synthetic cannabinoid with similar potency to compounds such as MDMB-FUBINACA and 5F-ADB, which have been responsible for numerous fatal and non-fatal drug overdoses, consistent with previously reported compounds from the patent literature showing bromination of the indazole ring at the 5-, 6-, or 7- positions to increase potency over the unsubstituted analogues. ADB-5'Br-PINACA is the 5'-bromo analog of ADB-PINACA. Synthesis ADB-5'Br-PINACA can be synthesized from a "half finished" synthesis precursor known as ADB-5-Br-INACA, related to MDMB-5Br-INACA. Legality ADB-5'Br-PINACA is not specifically sched ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AM-630
AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2, with a ''K''i of 32.1 nM at CB2 and 165x selectivity over CB1, at which it acted as a weak partial agonist. It is used in the study of CB2 mediated responses and has been used to investigate the possible role of CB2 receptors in the brain. AM-630 is significant as one of the first indole derived cannabinoid ligands substituted on the 6-position of the indole ring, a position that has subsequently been found to be important in determining affinity and efficacy at both the CB1 and CB2 receptors, and has led to the development of many related derivatives. See also * AM-1221 * Pravadoline * WIN 54,461 WIN 54,461 (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2. See also * ADB-5'Br-PINACA * AM-630 (6-Iodopravadoline) * WIN 48,098 (Pravadoline) * WIN 55,212-2 References ... ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WIN 48,098
Pravadoline (WIN 48,098) is an anti-inflammatory and analgesic drug with an IC50 of 4.9 μM and a ''K''i of 2511 nM at CB1, related in structure to nonsteroidal anti-inflammatory drugs (NSAIDs) such as indometacin. It was developed in the 1980s as a new antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX). However, pravadoline was found to exhibit unexpectedly strong analgesic effects, which appeared at doses ten times smaller than the effective anti-inflammatory dose and so could not be explained by its action as a COX inhibitor. These effects were not blocked by opioid antagonists such as naloxone, and it was eventually discovered that pravadoline represented the first compound from a novel class of cannabinoid agonists, the aminoalkylindoles. Pravadoline was never developed for use as an analgesic, partly due to toxicity concerns (although these were later shown to be a result of the salt form that t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 MAP kinase, p42 and p44 MAP kinase, p44 MAP kinase via receptor-mediated signaling. At 5 μM WIN 55,212-2 inhibits Adenosine Triphosphate, ATP production in sperm in a CB1 receptor, CB1 receptor-dependent fashion. WIN 55,212-2, along with HU-210 and JWH-133, may prevent the inflammation caused by amyloid beta proteins involved in Alzheimer's disease, in addition to preventing cognitive impairment and loss of neuronal genetic markers, markers. This anti-inflammatory action is induced through agonist action at cannabinoid receptors, which prevents microglial activation that elicits the inflammation. WIN 55,212-2 is a ful ... [...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] |
WIN Compounds
Win or WIN most likely refers to: * A victory Win, Winning, WIN or Winner may also refer to: Arts and entertainment Film * '' Win!'', a 2016 American film Literature * ''Win'' (Coben novel), 2021 * WIN (pacifist magazine) * WIN (wrestling magazine), US Music * Win (band), a Scottish band * "Win" (song), by Jay Rock * "Win", a song by Ateez from the album '' Treasure EP.Fin: All to Action'' * "Win", a song by Brian McKnight from the album ''Gold'' * "Win", a song by David Bowie from the album ''Young Americans'' * "Win", a song by Stefflon Don and DJ Khaled from the mixtape '' Secure'' * Worldwide Independent Network (WIN), a coalition of independent music bodies, see Independent record label#Worldwide Independent Network (WIN)) Television and radio * Win Radio, a Philippine radio network ** 91.5 Win Radio, its flagship station * Win FM, an Indian radio station * WIN Television, an Australian television network ** WIN Corporation, the owner of WIN Television ** WIN News, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
