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Pravadoline
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 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] |
RCS-4
RCS-4, or 1-pentyl-3-(4-methoxybenzoyl)indole, is a synthetic cannabinoid drug sold under the names SR-19, BTM-4, or Eric-4 (later shortened to E-4), but originally, OBT-199. Pharmacology RCS-4 is a potent cannabinoid receptor agonist, with EC50 values of 146 nM for human CB1 receptors, and 46 nM for human CB2 receptors. All methoxyphenyl regioisomers, and ''N''-butyl homologues of RCS-4 and its regioisomers also display potent agonist activities at CB1 and CB2 receptors. Legality RCS-4 was banned in Sweden on 1 October 2010 as a hazardous good harmful to health, after being identified as an ingredient in "herbal" synthetic cannabis products. It was outlawed in Denmark on 11 March 2011. In August 2011, New Zealand added not only RCS-4 but also its 1-butyl homologue, and the 2-methoxybenzoyl isomers of both these compounds, to a temporary class drug schedule (i.e. equivalent to Class C but reviewed after 12 months, and with personal possession and use of small amounts decrimi ... [...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 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] |
Anti-inflammatory
Anti-inflammatory is the property of a substance or treatment that reduces inflammation, fever or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs reduce pain by inhibiting mechanisms of inflammation, as opposed to opioids, which affect the central nervous system to block pain. Common anti-inflammatory drugs include nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, antileukotrienes, and monoclonal antibodies. Drugs Clinically approved Nonsteroidal anti-inflammatory drugs NSAIDs alleviate pain by counteracting the cyclooxygenase (COX) enzyme involved in pain mechanisms. Some common examples of NSAIDs are aspirin, ibuprofen, and naproxen. Selective COX-2 inhibitors, such as celecoxib, block the enzymatic conversion of arachidonic acid into prostaglandin, inhibiting inflammation and pain. Analgesics commonly associated with anti-inflammatory drugs, such as acetaminophen (paracetamol), hav ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Brewer's Yeast
''Saccharomyces cerevisiae'' () (brewer's yeast or baker's yeast) is a species of yeast (single-celled fungal microorganisms). The species has been instrumental in winemaking, baking, and brewing since ancient times. It is believed to have been originally isolated from the skin of grapes. It is one of the most intensively studied eukaryotic model organisms in molecular and cell biology, much like ''Escherichia coli'' as the model bacterium. It is the microorganism which causes many common types of fermentation. ''S. cerevisiae'' cells are round to ovoid, 5–10 μm in diameter. It reproduces by budding. Many proteins important in human biology were first discovered by studying their homologs in yeast; these proteins include cell cycle proteins, signaling proteins, and protein-processing enzymes. ''S. cerevisiae'' is currently the only yeast cell known to have Berkeley bodies present, which are involved in particular secretory pathways. Antibodies against ''S. c ... [...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] |
Opioid Receptor
Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin receptors (SSTRs). Opioid receptors are distributed widely in the brain, in the spinal cord, on peripheral neurons, and digestive tract. Discovery By the mid-1960s, it had become apparent from pharmacologic studies that opioids were likely to exert their actions at specific receptor sites, and that there were likely to be multiple such sites. Early studies had indicated that opiates appeared to accumulate in the brain. The receptors were first identified as specific molecules through the use of binding studies, in which opiates that had been labeled with radioisotopes were found to bind to brain membrane homogenates. The first such study was published in 1971, using 3H- levorphanol. In 1973, Candace Pert and Solomon H. Snyder publi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bradykinin
Bradykinin (BK) (from Greek ''brady-'' 'slow' + ''-kinin'', ''kīn(eîn)'' 'to move') is a peptide that promotes inflammation. It causes arterioles to dilate (enlarge) via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpolarizing factor and makes veins constrict, via prostaglandin F2, thereby leading to leakage into capillary beds, due to the increased pressure in the capillaries. Bradykinin consists of nine amino acids, and is a physiologically and pharmacologically active peptide of the kinin group of proteins. A class of drugs called angiotensin-converting-enzyme inhibitors (ACE inhibitors) increase bradykinin levels by inhibiting its degradation, thereby increasing its blood pressure lowering effect. ACE inhibitors are FDA approved for the treatment of hypertension and heart failure. Structure Bradykinin, sometimes referred to as BK, is a 9–amino acid Translation (genetics), peptide chain. The amino acid sequence of bradykinin is: arginine, Arg-pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adjuvant
In pharmacology, an adjuvant is a drug or other substance, or a combination of substances, that is used to increase the efficacy or potency of certain drugs. Specifically, the term can refer to: * Adjuvant therapy in cancer management * Analgesic adjuvant in pain management * Immunologic adjuvant In immunology, an adjuvant is a substance that increases or modulates the immune response to a vaccine. The word "adjuvant" comes from the Latin word , meaning to help or aid. "An immunologic adjuvant is defined as any substance that acts to acce ... in vaccines {{sia Adjuvants ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
