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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 and p44 MAP kinase via receptor-mediated signaling. At 5 μM WIN 55,212-2 inhibits ATP production in sperm in a 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 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 full agonist at the CB1 cannabinoid receptor ( ''K''i = 1.9 nM) a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pancreatic Stellate Cell Cropped
The pancreas is an Organ (anatomy), organ of the digestive system and endocrine system of vertebrates. In humans, it is located in the abdominal cavity, abdomen behind the stomach and functions as a gland. The pancreas is a mixed or heterocrine gland, i.e. it has both an endocrine and a digestive exocrine function. 99% of the pancreas is exocrine and 1% is endocrine. As an endocrine gland, it functions mostly to regulate blood sugar levels, secreting the hormones insulin, glucagon, somatostatin, and pancreatic polypeptide. As a part of the digestive system, it functions as an exocrine gland secreting pancreatic juice into the duodenum through the pancreatic duct. This juice contains bicarbonate, which neutralizes acid entering the duodenum from the stomach; and digestive enzymes, which break down carbohydrates, proteins, and lipids, fats in food entering the duodenum from the stomach. Inflammation of the pancreas is known as pancreatitis, with common causes including chronic Alc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Genetic Markers
A genetic marker is a gene or DNA sequence with a known location on a chromosome that can be used to identify individuals or species. It can be described as a variation (which may arise due to mutation or alteration in the genomic loci) that can be observed. A genetic marker may be a short DNA sequence, such as a sequence surrounding a single base-pair change ( single nucleotide polymorphism, SNP), or a long one, like minisatellites. Background For many years, gene mapping was limited to identifying organisms by traditional phenotypes markers. This included genes that encoded easily observable characteristics such as blood types or seed shapes. The insufficient number of these types of characteristics in several organisms limited the mapping efforts that could be done. This prompted the development of gene markers which could identify genetic characteristics that are not readily observable in organisms (such as protein variation). Types Some commonly used types of genetic ma ... [...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 Bioinfor ... ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WIN 56,098
WIN 56,098 is a chemical that is considered to be an aminoalkylindole derivative. It is a tricyclic aryl derivative that acts as a competitive antagonist at the CB2 cannabinoid receptor. Its activity at CB1 was significantly less effective. WIN 56,098 failed to antagonize any of the ''in vivo'' effects of THC. See also * 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 canna ... * WIN 55,225 References Cannabinoids Aminoalkylindoles WIN compounds 4-Morpholinyl compunds Anthracenes {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WIN 55,225
JWH-200 (WIN 55,225) is an analgesic chemical from the aminoalkylindole family that acts as a cannabinoid receptor agonist. Its Dissociation constant, binding affinity, ''K''i at the CB1 receptor is 42 nM, around the same as that of THC, but its analgesic potency ''in vivo'' was higher than that of other analogues with stronger CB1 binding affinity ''in vitro'', around 3 times that of THC but with less sedative effect, most likely reflecting favourable pharmacokinetic characteristics. It was discovered in 1991 by Sterling Drug as a potential analgesic following the earlier identification of related compounds such as pravadoline and WIN 55,212-2. Legal status Australia JWH-200 is considered a Schedule 9 prohibited substance in Australia under the Standard for the Uniform Scheduling of Medicines and Poisons, Poisons Standard (October 2015). A Schedule 9 substance is a substance which may be abused or misused, the manufacture, possession, sale or use of which should be prohibite ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 * AM-630 (6-Iodopravadoline) * WIN 48,098 (Pravadoline) * 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 canna ... References Cannabinoids Aminoalkylindoles WIN compounds Benzoylindoles 4-Morpholinyl compunds Organobromides {{cannabinoid-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
WIN 48,098
Pravadoline (WIN 48,098) is an antinflammatory 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 th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Schedule I Controlled Substance
This is the list of Schedule I drugs as defined by the United States Controlled Substances Act. 21 CFRbr>1308.11(CSA Sched I) with changes through (Oct 18, 2012). Retrieved September 6, 2013. The following findings are required for drugs to be placed in this schedule: # The drug or other substance has a high potential for abuse. # The drug or other substance has no currently accepted medical use in treatment in the United States. # There is a lack of accepted safety for use of the drug or other substance under medical supervision. Except as specifically authorized, it is illegal for any person: # to manufacture, distribute, or dispense, or possess with intent to manufacture, distribute, or dispense, a controlled substance; or # to create, distribute, dispense, or possess with intent to distribute or dispense, a counterfeit substance. Additional substances are added to the list by the Secretary of Health and Human Services pursuant to 21 CFR 1308.49. [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peroxisome Proliferator-activated Receptor Gamma
Peroxisome proliferator- activated receptor gamma (PPAR-γ or PPARG), also known as the glitazone reverse insulin resistance receptor, or NR1C3 (nuclear receptor subfamily 1, group C, member 3) is a type II nuclear receptor functioning as a transcription factor that in humans is encoded by the ''PPARG'' gene. Tissue distribution PPARG is mainly present in adipose tissue, colon and macrophages. Two isoforms of PPARG are detected in the human and in the mouse: PPAR-γ1 (found in nearly all tissues except muscle) and PPAR-γ2 (mostly found in adipose tissue and the intestine). Gene expression This gene encodes a member of the peroxisome proliferator-activated receptor (PPAR) subfamily of nuclear receptors. PPARs form heterodimers with retinoid X receptors (RXRs) and these heterodimers regulate transcription of various genes. Three subtypes of PPARs are known: PPAR-alpha, PPAR-delta, and PPAR-gamma. The protein encoded by this gene is PPAR-gamma and is a regulator of adipocyte ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peroxisome Proliferator-activated Receptor Alpha
Peroxisome proliferator-activated receptor alpha (PPAR-α), also known as NR1C1 (nuclear receptor subfamily 1, group C, member 1), is a nuclear receptor protein functioning as a transcription factor that in humans is encoded by the ''PPARA'' gene. Together with peroxisome proliferator-activated receptor delta and peroxisome proliferator-activated receptor gamma, PPAR-alpha is part of the subfamily of peroxisome proliferator-activated receptors. It was the first member of the PPAR family to be cloned in 1990 by Stephen Green and has been identified as the nuclear receptor for a diverse class of rodent hepatocarcinogens that causes proliferation of peroxisomes. Expression PPAR-α is primarily activated through ligand binding. Endogenous ligands include fatty acids such as arachidonic acid as well as other polyunsaturated fatty acids and various fatty acid-derived compounds such as certain members of the 15-hydroxyeicosatetraenoic acid family of arachidonic acid metabolites, e.g ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
