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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] |
Nociceptin Receptor
The nociceptin opioid peptide receptor (NOP), also known as the nociceptin/orphanin FQ (N/OFQ) receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the ''OPRL1'' (opioid receptor-like 1) gene. The nociceptin receptor is a member of the opioid subfamily of G protein-coupled receptors whose natural Ligand (biochemistry), ligand is the 17 amino acid neuropeptide known as nociceptin, nociceptin (N/OFQ). This receptor is involved in the regulation of numerous brain activities, particularly instinctive and emotional behaviors. Antagonists targeting NOP are under investigation for their role as treatments for depression and Parkinson's disease, whereas NOP agonists have been shown to act as powerful, non-addictive painkillers in non-human primates. Although NOP shares high sequence identity (~60%) with the ‘classical’ opioid receptors Μ-opioid receptor, μ-OP (MOP), Κ-opioid receptor, κ-OP (KOP), and Δ-opioid receptor, δ-OP (DOP), it possesses litt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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] |
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] |
Partial Agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (biochemistry), ligands which display both agonistic and Receptor antagonist, antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspi ... [...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] |
Homologous Series
In organic chemistry, a homologous series is a sequence of compounds with the same functional group and similar chemical properties in which the members of the series differ by the number of repeating units they contain. This can be the length of a carbon chain, for example in the straight-chained alkanes (paraffins), or it could be the number of monomers in a homopolymer such as amylose. A homologue (also spelled as homolog) is a chemical compound, compound belonging to a homologous series. Compounds within a homologous series typically have a fixed set of functional groups that gives them similar chemical and physical properties. (For example, the series of primary straight-chained alcohols has a hydroxyl at the end of the carbon chain.) These properties typically change gradually along the series, and the changes can often be explained by mere differences in molecular size and mass. The name "homologous series" is also often used for any collection of compounds that have similar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Buprenorphine
Buprenorphine, sold under the brand name Subutex among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), or as an implant. For opioid use disorder, the patient must have moderate opioid withdrawal symptoms before buprenorphine can be administered under direct observation of a health-care provider. In the United States, the combination formulation of buprenorphine/naloxone (Suboxone) is usually prescribed to discourage misuse by injection. However, more recently the efficacy of naloxone in preventing misuse has been brought into question, and preparations of buprenorphine combined with naloxone could potentially be less safe than buprenorphine alone. Maximum pain relief is generally within an hour with effects up to 24 hours. Buprenorphine affects different types of opioid receptors in diffe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterocyclic Compounds With 6 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] |
Oxygen Heterocycles
Oxygen is a chemical element; it has symbol O and atomic number 8. It is a member of the chalcogen group in the periodic table, a highly reactive nonmetal, and a potent oxidizing agent that readily forms oxides with most elements as well as with other compounds. Oxygen is the most abundant element in Earth's crust, making up almost half of the Earth's crust in the form of various oxides such as water, carbon dioxide, iron oxides and silicates.Atkins, P.; Jones, L.; Laverman, L. (2016).''Chemical Principles'', 7th edition. Freeman. It is the third-most abundant element in the universe after hydrogen and helium. At standard temperature and pressure, two oxygen atoms will bind covalently to form dioxygen, a colorless and odorless diatomic gas with the chemical formula . Dioxygen gas currently constitutes approximately 20.95% molar fraction of the Earth's atmosphere, though this has changed considerably over long periods of time in Earth's history. A much rarer triat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrogen Heterocycles
Nitrogen is a chemical element; it has symbol N and atomic number 7. Nitrogen is a nonmetal and the lightest member of group 15 of the periodic table, often called the pnictogens. It is a common element in the universe, estimated at seventh in total abundance in the Milky Way and the Solar System. At standard temperature and pressure, two atoms of the element bond to form N2, a colourless and odourless diatomic gas. N2 forms about 78% of Earth's atmosphere, making it the most abundant chemical species in air. Because of the volatility of nitrogen compounds, nitrogen is relatively rare in the solid parts of the Earth. It was first discovered and isolated by Scottish physician Daniel Rutherford in 1772 and independently by Carl Wilhelm Scheele and Henry Cavendish at about the same time. The name was suggested by French chemist Jean-Antoine-Claude Chaptal in 1790 when it was found that nitrogen was present in nitric acid and nitrates. Antoine Lavoisier suggested instead the nam ... [...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] |
