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LY-88329
LY-88329 is an opioid receptor ligand related to medicines such as pethidine. It has high affinity to the μ-opioid receptor, but unlike structurally related drugs such as 3-methylfentanyl and OPPPP, LY-88329 is a potent opioid antagonist. In animal studies it blocks the effects of morphine and has anorectic An anorectic is a drug that reduces appetite, resulting in lower food consumption, leading to weight loss. These substances work by affecting the central nervous system or certain neurotransmitters to create a feeling of fullness or reduce the desi ... action. See also * Alvimopan References Mu-opioid receptor antagonists 3-Hydroxyphenyl compounds 4-Phenylpiperidines {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alvimopan
Alvimopan (trade name Entereg) is a drug which behaves as a peripherally acting μ-opioid receptor antagonist. With the limited ability to cross the blood–brain barrier and reach the μ-opioid receptors of the central nervous system, the clinically undesirable effects of centrally acting opioid antagonists (like reversal of opioid-mediated analgesia) are avoided without affecting the intended blockade of μ-opioid receptors in the gastrointestinal tract. It is currently only Food and Drug Administration approved for the treatment of postoperative ileus which it received in May 2008. Medical uses Alvimopan is indicated in people to avoid postoperative ileus following partial large or small bowel resection with primary anastomosis. Alvimopan accelerates the gastrointestinal recovery period as defined by time to first bowel movement or flatus.Alvimopan Product Label as approved by the FDA on May 20, 2008. Adverse effects There is a potential risk of myocardial infarction in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
OPPPP
OPPPP (1-(3-Oxo-3-phenylpropyl)-4-phenyl-4-piperidinyl propionate) is one of several compounds derived from MPPP, the reversed ester of the opioid analgesic pethidine, which were sold as designer drugs in the 1980s, but have been rarely encountered by law enforcement since the passage of the Federal Analogue Act in 1986. In animal studies it was found to be around 1000× the potency of pethidine, making it several times the potency of fentanyl and with similar hazards of respiratory depression and overdose. It is closely related to numerous compounds made by Janssen et al. for which the structure-activity relationship is well established. See also * List of fentanyl analogues * PEPAP * LY-88329 LY-88329 is an opioid receptor ligand related to medicines such as pethidine. It has high affinity to the μ-opioid receptor, but unlike structurally related drugs such as 3-methylfentanyl and OPPPP, LY-88329 is a potent opioid antagonist. In a ... References 4-Phenylpiperidin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, including analgesic, pain relief. The terms "opioid" and "opiate" are sometimes used interchangeably, but the term "opioid" is used to designate all substances, both natural and synthetic, that bind to opioid receptors in the brain. Opiates are alkaloid compounds naturally found in the opium poppy plant ''Papaver somniferum''. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, and Cold medicine, suppressing cough. The opioid receptor antagonist naloxone is used to reverse opioid overdose. Extremely potent opioids such as carfentanil are approved only for Veterinary medicine, veterinary use. Opioids are also frequently use ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pethidine
Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a fully synthetic opioid pain medication of the phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized by Otto Schaumann while working for IG Farben, in Germany. Pethidine is the prototype of a large family of analgesics including the pethidine 4-phenylpiperidines (e.g., piminodine, anileridine), the prodines (e.g., alphaprodine, MPPP), bemidones (e.g., ketobemidone), and others more distant, including diphenoxylate and analogues. Pethidine is indicated for the treatment of moderate to severe pain, and is delivered as a hydrochloride salt in tablets, as a syrup, or by intramuscular, subcutaneous, or intravenous injection. For much of the 20th century, pethidine was the opioid of choice for many physicians; in 1975, 60% of doctors prescribed it for acute pain and 22% for chroni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
μ-opioid Receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical μ-opioid receptor agonist is morphine, the primary psychoactive alkaloid in opium and for which the receptor was named, with Mu (letter), mu being the first letter of Morpheus, the compound's namesake in the original Greek. It is an inhibitory G-protein coupled receptor that activates the Gi alpha subunit, Gi alpha subunit, inhibiting adenylate cyclase activity, lowering Cyclic adenosine monophosphate, cAMP levels. Structure The structure of the inactive μ-opioid receptor has been determined with the antagonists Beta-Funaltrexamine, β-FNA and alvimopan. Many structures of the active state are also available, with agonists including DAMGO, Β-Endorphin, β-endorphin, fentanyl and morphine. The structure with the agonist BU72 has the h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3-methylfentanyl
3-Methylfentanyl (3-MF, mefentanyl) is an opioid analgesic that is an analog of fentanyl. 3-Methylfentanyl is one of the most potent opioids, estimated to be between 400 and 6000 times stronger than morphine, depending on which isomer is used (with the cis isomers being the more potent ones). Overview and history was first discovered in 1974 and subsequently appeared on the street as an alternative to the clandestinely produced fentanyl analog α-methylfentanyl. However, it quickly became apparent that was much more potent than α-methylfentanyl, and correspondingly more dangerous. While was initially sold on the black market for only a short time between 1984 and 1985, its high potency made it an attractive target to clandestine drug producers, as racemic is 10–15 times more potent than fentanyl, and so correspondingly larger amounts of cut product for street sales can be produced for an equivalent amount of effort as for producing fentanyl itself; one gram of mig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid Antagonist
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the opioid receptors with higher affinity than agonists but do not activate the receptors. This effectively blocks the receptor, preventing the body from responding to opioids and endorphins. Some opioid antagonists are not pure antagonists but do produce some weak opioid partial agonist effects, and can produce analgesic effects when administered in high doses to opioid-naive individuals. Examples of such compounds include nalorphine and levallorphan. However, the analgesic effects from these specific drugs are limited and tend to be accompanied by dysphoria, most likely due to additional agonist action at the κ-opioid receptor. As they induce opioid withdrawal effects in people who are taking, or have recently used, opioid full agoni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morphine
Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are multiple methods used to administer morphine: oral; sublingual administration, sublingual; via inhalation; intramuscular, injection into a muscle, Subcutaneous injection, injection under the skin, or injection into the spinal cord area; transdermal; or via rectal administration, rectal suppository. It acts directly on the central nervous system (CNS) to induce analgesia and alter perception and emotional response to pain. Physical and psychological dependence and tolerance may develop with repeated administration. It can be taken for both acute pain and chronic pain and is frequently used for pain from myocardial infarction, kidney stones, and during Childbirth, labor. Its maximum effect is reached after about 20 minutes when administ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anorectic
An anorectic is a drug that reduces appetite, resulting in lower food consumption, leading to weight loss. These substances work by affecting the central nervous system or certain neurotransmitters to create a feeling of fullness or reduce the desire to eat. The understanding of anorexiant effects is crucial in the development of interventions for weight management, eating disorders, and related health concerns. The anorexiant effect can be induced through diverse mechanisms, ranging from hormonal regulation to neural signaling. Ghrelin, leptin, and peptide YY are among the hormones involved in appetite control. Additionally, neurotransmitters such as serotonin and dopamine in the central nervous system contribute significantly to the regulation of food intake. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek and ), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
