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BU-48
BU-48 is a drug that is used in scientific research. It is from the oripavine family, related to better-known drugs such as etorphine and buprenorphine. The parent compound from which BU-48 was derived (with ''N''-methyl rather than methylcyclopropyl on the nitrogen and lacking the aliphatic hydroxyl group) is a powerful μ-opioid agonist 1000 times more potent than morphine, but in contrast BU-48 has only weak analgesic effects and instead acts primarily as a δ-opioid agonist. Its main effects are to produce convulsions, but it may also have antidepressant Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathi ... effects. See also * BU72 * BU08028 References Semisynthetic opioids Delta-opioid receptor agonists Hydroxyarenes 4,5-Epoxymorphinans Heterocyclic compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semisynthetic Opioids
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] |
BU72
BU72 is an extremely potent opioid used in pharmacological research. Pharmacology BU72 is an agonist for the μ-opioid receptor with exceptionally high binding affinity and Potency (pharmacology), potency, comparable to carfentanil. It also has extremely high Efficacy (pharmacology), efficacy, giving a stronger maximal effect than the standard full agonist DAMGO. In animal studies, it was found to be a Potency (pharmacology), potent analgesic, analgesic (giving pain relief at very low doses), with a slow Onset of action, onset and long Pharmacodynamics, duration of action. Chemistry BU72 was used to produce the first crystal structure of the active μ-opioid receptor, and is now widely used to model the activation process. The stereochemistry has recently been revised, with the phenyl group in the (''R'') Absolute configuration, configuration. In the crystal structure, BU72 appears to bond to the receptor Covalent bond, covalently, but this seems not to occur , since the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BU08028
BU08028 is a drug which acts as an extremely potent partial agonist at both the μ-opioid receptor and nociceptin receptor. It is a homologue of buprenorphine extended by just one carbon on the side chain, but has relatively greater activity at the nociceptin receptor, which is thought to reduce the abuse potential without compromising analgesia. See also * BU-48 * BU72 BU72 is an extremely potent opioid used in pharmacological research. Pharmacology BU72 is an agonist for the μ-opioid receptor with exceptionally high binding affinity and Potency (pharmacology), potency, comparable to carfentanil. It also ... References Mu-opioid receptor agonists Heterocyclic compounds with 6 rings Oxygen heterocycles Nitrogen heterocycles Cyclopropyl compounds Alcohols {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopropyl Compounds
A cyclopropyl group is a chemical structure derived from cyclopropane; it is typically produced in a cyclopropanation reaction. The group has an empirical formula of C3H5 and chemical bonds from each of the three carbons to both of the other two. Structure and bonding Due to the unfavoured bond angles (60°), cyclopropyl groups are highly strained. Two orbital models were proposed to describe the bonding situation. The Coulson-Moffit model uses bent bonds. The C-C bonds are formed by overlap of two sp-hybrid orbitals. To adapt to the small bond angle, there is some rehybridization resulting in sp~5-hybrids for the ring bonds and sp~2 for the C-H bonds. This model resembles the banana bond model for C=C double bonds (τ bonds). Alternatively the structure can be explained with the Walsh model. Here the two sp-hybrids forming the ring bond are separated into one sp2-hybrid and one pure p-orbital. This corresponds to the π bond description of C=C double bonds. Cyclopropyl grou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterocyclic Compounds With 7 Or More Rings
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic organic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of organic heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of organic heterocyclic chemistry focuses especially on organic unsaturated derivatives, and the preponderance of work and applications involves unstrained organic 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of organic heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of pyridin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxyarenes
Phenol (also known as carbolic acid, phenolic acid, or benzenol) is an aromatic organic compound with the molecular formula . It is a white crystalline solid that is volatile and can catch fire. The molecule consists of a phenyl group () bonded to a hydroxy group (). Mildly acidic, it requires careful handling because it can cause chemical burns. It is acutely toxic and is considered a health hazard. Phenol was first extracted from coal tar, but today is produced on a large scale (about 7 million tonnes a year) from petroleum-derived feedstocks. It is an important industrial commodity as a precursor to many materials and useful compounds, and is a liquid when manufactured. It is primarily used to synthesize plastics and related materials. Phenol and its chemical derivatives are essential for production of polycarbonates, epoxies, explosives such as picric acid, Bakelite, nylon, detergents, herbicides such as phenoxy herbicides, and numerous pharmaceutical dru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oripavine
Oripavine is an opioid and the major metabolite of thebaine. It is the precursor to the semi-synthetic compounds etorphine and buprenorphine. Although this chemical compound has analgesic potency comparable to morphine, it is not used clinically due to severe adverse effects and a low therapeutic index. Being a precursor to a series of extremely strong opioids, oripavine is a controlled substance in some jurisdictions. Pharmacological properties Oripavine possesses an analgesic potency comparable to morphine; however, it is not clinically useful due to severe toxicity and low therapeutic index. In both mice and rats, toxic doses caused tonic-clonic seizures followed by death, similar to thebaine. Oripavine has a potential for dependence which is significantly greater than that of thebaine but slightly less than that of morphine. Bridged derivatives (The Bentley compounds) Of much greater relevance are the properties of the orvinols, a large family of semi-synthet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etorphine
Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the related plants '' Papaver orientale'' and '' Papaver bracteatum''. It was reproduced in 1963 by a research group at MacFarlan Smith in Edinburgh, led by Kenneth Bentley. It can be produced from thebaine. Veterinary use Etorphine is available legally only for veterinary use and is strictly governed by law. It is often used to immobilise elephants and other large mammals. Diprenorphine (Revivon) is an opioid receptor antagonist that can be administered in proportion to the amount of etorphine used (1.3 times) to reverse its effects. Veterinary-strength etorphine is fatal to humans. For this reason the package as supplied to vets always includes the human antidote along with the etorphine. The human antidote is generally naloxone, not dipr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathisia, sexual dysfunction, and emotional blunting. There is an increased risk of Suicidal ideation, suicidal thinking and Suicide, behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome, which resembles recurrent Depression (mood), depression in the case of the Selective serotonin reuptake inhibitor, SSRI class, may occur after stopping the intake of any antidepressant. Research regarding the effectiveness of antidepressants for depression in adults is controversial and has found both benefits and drawbacks. Meanwhile, evidence of benefit in children and adolescents is unclear, even though antidepressant use has considerably increased in children and adolescents in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convulsion
A convulsion is a medical condition where the body muscles contract and relax rapidly and repeatedly, resulting in uncontrolled shaking. Because epileptic seizures typically include convulsions, the term ''convulsion'' is often used as a synonym for ''seizure''. However, not all epileptic seizures result in convulsions, and not all convulsions are caused by epileptic seizures. Non-epileptic convulsions have no relation with epilepsy, and are caused by non-epileptic seizures. Convulsions can be caused by epilepsy, infections (including a severe form of listeriosis which is caused by eating food contaminated by Listeria monocytogenes), brain trauma, or other medical conditions. They can also occur from an electric shock or improperly enriched air for scuba diving. The word ''fit'' is sometimes used to mean a convulsion or epileptic seizure. Signs and symptoms A person having a convulsion may experience several different symptoms, such as a brief blackout, confusion, drooling, l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
