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Ciramadol
Ciramadol (WY-15,705) is an opioid analgesic that was developed in the late 1970s and is related to phencyclidine, tramadol, tapentadol and venlafaxine. It is a mixed agonist-antagonist for the μ-opioid receptor with relatively low abuse potential and a ceiling on respiratory depression which makes it a relatively safe drug. It has a slightly higher potency and effectiveness as an analgesic than codeine, but is weaker than morphine. Other side effects include sedation and nausea but these are generally less severe than with other similar drugs. Synthesis The Claisen-Schmidt condensation between 3-(methoxymethoxy)benzaldehyde 3709-05-2(1) and cyclohexanone (2) affordeCID:54364197(3). Michael addition of dimethylamine Dimethylamine is an organic compound with the formula (CH3)2NH. This secondary amine is a colorless, flammable gas with an ammonia-like odor. Dimethylamine is commonly encountered commercially as a solution in water at concentrations up to around ... leads t ... [...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] |
Profadol
Profadol (CI-572) is an opioid analgesic which was developed in the 1960s by Parke-Davis. It acts as a mixed agonist-antagonist of the μ-opioid receptor. The analgetic potency is about the same as of pethidine (meperidine), the antagonistic effect is 1/50 of nalorphine. Synthesis The Knoevenagel condensation between 3'-Methoxybutyrophenone 1550-06-1and Ethyl cyanoacetate gives (1). Conjugate addition of cyanide gives (2). Hydrolysis of both nitrile groups, saponification of the ester and decarboxylation gives the diacidCID:164137621(3). Imide formation occurs upon treatment with methylamine giving 3-(3-Methoxyphenyl)-1-methyl-3-propylpyrrolidine-2,5-dioneCID:163444474(4). Reduction of the imide by lithium aluminium hydride gave 505-32-429369-01-5] (5). Demethylation completed the synthesis of Profadol (6). See also * BDPC, Bromadol * C-8813 * Ciramadol * Faxeladol * Prodilidine * Tapentadol * Tramadol Tramadol, sold under the brand name Tramal among others, is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
C-8813
C-8813 (thiobromadol) is a potent μ-opioid receptor agonist with a distinctive chemical structure which is not closely related to other established families of opioid drugs. The ''trans''-isomer was found to be around 591 times more potent than morphine in animal studies. The same study assigned a potency of 504 times that of morphine to the related compound BDPC. C-8813 is claimed to be similarly potent at the δ-opioid receptor, which antagonizes the μ-induced depression of breathing, presumably making the drug safer. C-8813 has never been approved for use in humans. See also * BDPC * Ciramadol * Faxeladol * Profadol * Tapentadol * Tramadol Tramadol, sold under the brand name Tramal among others, is an opioid analgesic, pain medication and a serotonin–norepinephrine reuptake inhibitor (SNRI) used to treat moderately severe pain. When taken by mouth in an immediate-release form ... References Arylcyclohexylamines Synthetic opioids Thiophenes Tert ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bromadol
BDPC (systematic name 4-(4-bromophenyl)-4-(dimethylamino)-1-(2-phenylethyl)cyclohexanol; also known as bromadol) is a potent fully synthetic opioid with a distinctive arylcyclohexylamine chemical structure. It was developed by Daniel Lednicer at Upjohn in the 1970s. Initial studies estimated that it was around 10,000 times the potency of morphine in animal models. However, later studies using more modern techniques assigned a value of 504 times the potency of morphine for the more active ''trans''-isomer. This drug was first seized along with three kilograms of acetylfentanyl in an April 25, 2013 police action in Montreal, Canada, and has reportedly continued to be available on the designer drug market internationally. Analogues where the ''para''-bromine is replaced by chlorine or a methyl group retain similar activity, while the ''meta''-hydroxyl derivative demonstrated robust antagonist activity. ] ] See also * 3-HO-PCP * 4-Keto-PCP * C-8813 * Cebranopadol * Ciramadol * Di ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tramadol
Tramadol, sold under the brand name Tramal among others, is an opioid analgesic, pain medication and a serotonin–norepinephrine reuptake inhibitor (SNRI) used to treat moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It is available in combination with paracetamol (acetaminophen). As is typical of opioids, common side effects include constipation, pruritis, itchiness, and nausea. Serious side effects may include hallucinations, seizures, increased risk of serotonin syndrome, decreased alertness, and drug addiction. A change in dosage may be recommended in those with chronic kidney disease, kidney or liver problems. It is not recommended in those who are at risk of suicide or in those who are pregnant. While not recommended in women who are breastfeeding, those who take a single dose should not generally have to stop breastfeeding. Tramadol is converted ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tapentadol
Tapentadol, sold under the brand names Nucynta and Palexia among others, is a synthetic opioid analgesic with a dual mode of action as a highly selective full agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Tapentadol is used medically for the treatment of moderate to severe pain. It is highly addictive and is a commonly abused drug. Common side effects include euphoria, constipation, nausea, vomiting, headaches, loss of appetite, drowsiness, dizziness, itching, dry mouth, and sweating. Serious side effects may include addiction and dependence, substance abuse, respiratory depression and an increased risk of serotonin syndrome. Combining tapentadol with certain substances, including serotonergic drugs or other central nervous system depressants such as alcohol, cannabis, benzodiazepines, and other opioids, may increase the risk of serotonin syndrome, sedation, respiratory depression, and death. Analgesia occurs within 32 minutes of oral ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Faxeladol
Faxeladol (INN, USAN) (code names GRTA-9906, GRTA-0009906, EM-906, GCR-9905, GRT-TA300) is an opioid analgesic which was developed by Grünenthal GmbH but was never marketed for medical use anywhere in the world. It is related to tramadol and ciramadol, and was developed shortly after tramadol in the late 1970s. Similarly to tramadol, it was believed faxeladol would have analgesic, as well as antidepressant effects, due to its action on serotonin and norepinephrine reuptake. In various studies in the 1970s alongside tramadol, faxeladol was seen to be slightly more potent than tramadol, but with a higher rate of sudden seizures than tramadol, which is known to cause seizures without warning in some users. See also * Bromadol * Profadol Profadol (CI-572) is an opioid analgesic which was developed in the 1960s by Parke-Davis. It acts as a mixed agonist-antagonist of the μ-opioid receptor. The analgetic potency is about the same as of pethidine (meperidine), the antagonistic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimethylamine
Dimethylamine is an organic compound with the formula (CH3)2NH. This secondary amine is a colorless, flammable gas with an ammonia-like odor. Dimethylamine is commonly encountered commercially as a solution in water at concentrations up to around 40%. An estimated 270,000 tons were produced in 2005. Structure and synthesis The molecule consists of a nitrogen atom with two methyl substituents and one hydrogen. Dimethylamine is a weak base and the pKa of the ammonium CH3--CH3 is 10.73, a value above methylamine (10.64) and trimethylamine (9.79). Dimethylamine reacts with acids to form salts, such as dimethylamine hydrochloride, an odorless white solid with a melting point of 171.5 °C. Dimethylamine is produced by catalytic reaction of methanol and ammonia at elevated temperatures and high pressure: : Natural occurrence Dimethylamine is found quite widely distributed in animals and plants, and is present in many foods at the level of a few mg/kg. Uses Dimethylamine is a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
