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BU72
BU72 is an extremely potent opioid, with one of the highest known affinities for the μ-opioid receptor. In animal studies, it was found to be a potent analgesic, with a slow onset and long duration of action, but was not considered suitable to develop for medical use. It 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'') configuration, which has been accepted by the authors of the crystal structure. See also * 7-PET * Buprenorphine Buprenorphine 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 ... * BU-48 * BU08028 References Mu-opioid receptor agonists Nitrogen heterocycles Heterocyclic compounds with 6 rings [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
7-PET
7-PET is an opioid analgesic drug that has 300 times the potency of morphine by weight. It was discovered by K.W. Bentley and is related to the more well known oripavine derivative etorphine, which is used as a veterinary painkiller and anesthetic medication for the sedation of large animals such as elephants, giraffes, and rhinos. 7-PET itself has a 3-''O''-methyl ether which reduces potency, but the 3-OH derivative is around 2200 times more potent than morphine, almost the same potency as etorphine as a μ agonist, and unexpectedly the 3-hydrogen compound is also around the same potency of 2000 times morphine. Unlike etorphine, 7-PET is not controlled under the UN drug conventions, but it might still be considered to be a controlled substance analogue of etorphine on the grounds of its related chemical structure in some jurisdictions such as the United States, Canada, Australia, and New Zealand. See also * 14-Cinnamoyloxycodeinone * 14-Phenylpropoxymetopon * BU72 * ''N'' ... [...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. It is an inhibitory G-protein coupled receptor that activates the Gi alpha subunit, inhibiting adenylate cyclase activity, lowering cAMP levels. Structure The structure of the μ-opioid receptor has been determined with the antagonist β-FNA, the agonist BU72, and in a complex with DAMGO and Gi protein. Splice variants Three variants of the μ-opioid receptor are well characterized, though RT-PCR has identified up to 10 total splice variants in humans. Location They can exist either presynaptically or postsynaptically depending upon cell types. The μ-opioid receptors exist mostly presynaptically in the periaqueductal gray region, and in the superfi ... [...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 effects. See also * BU72 BU72 is an extremely potent opioid, with one of the highest known affinities for the μ-opioid receptor. In animal studies, it was found to be a potent analgesic, with a slow onset and long duration of action, but was not considered suitable to ... * BU08028 References Semisynthetic opioids Delta-opioid receptor agonists Phenols 4,5-Epoxymorphinans {{nervous-system-drug-s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BU08028
BU08028 is a drug which acts as a 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, with one of the highest known affinities for the μ-opioid receptor. In animal studies, it was found to be a potent analgesic, with a slow onset and long duration of action, but was not considered suitable to ... References {{pharm-stub Mu-opioid receptor agonists Heterocyclic compounds with 6 rings Oxygen heterocycles Nitrogen heterocycles Cyclopropanes Alcohols ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Crystal Structure
In crystallography, crystal structure is a description of the ordered arrangement of atoms, ions or molecules in a crystal, crystalline material. Ordered structures occur from the intrinsic nature of the constituent particles to form symmetric patterns that repeat along the principal directions of Three-dimensional space (mathematics), three-dimensional space in matter. The smallest group of particles in the material that constitutes this repeating pattern is the unit cell of the structure. The unit cell completely reflects the symmetry and structure of the entire crystal, which is built up by repetitive Translation (geometry), translation of the unit cell along its principal axes. The translation vectors define the nodes of the Bravais lattice. The lengths of the principal axes, or edges, of the unit cell and the angles between them are the lattice constants, also called ''lattice parameters'' or ''cell parameters''. The symmetry properties of the crystal are described by the con ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stereochemistry
Stereochemistry, a subdiscipline of chemistry, involves the study of the relative spatial arrangement of atoms that form the structure of molecules and their manipulation. The study of stereochemistry focuses on the relationships between stereoisomers, which by definition have the same molecular formula and sequence of bonded atoms (constitution), but differ in structural formula (the three-dimensional orientations of their atoms in space). For this reason, it is also known as 3D chemistry—the prefix "stereo-" means "three-dimensionality". Stereochemistry spans the entire spectrum of organic, inorganic, biological, physical and especially supramolecular chemistry. Stereochemistry includes methods for determining and describing these relationships; the effect on the physical or biological properties these relationships impart upon the molecules in question, and the manner in which these relationships influence the reactivity of the molecules in question ( dynamic stereochemis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenyl Group
In organic chemistry, the phenyl group, or phenyl ring, is a cyclic group of atoms with the formula C6 H5, and is often represented by the symbol Ph. Phenyl group is closely related to benzene and can be viewed as a benzene ring, minus a hydrogen, which may be replaced by some other element or compound to serve as a functional group. Phenyl group has six carbon atoms bonded together in a hexagonal planar ring, five of which are bonded to individual hydrogen atoms, with the remaining carbon bonded to a substituent. Phenyl groups are commonplace in organic chemistry. Although often depicted with alternating double and single bonds, phenyl group is chemically aromatic and has equal bond lengths between carbon atoms in the ring. Nomenclature Usually, a "phenyl group" is synonymous with C6H5− and is represented by the symbol Ph or, archaically, Φ. Benzene is sometimes denoted as PhH. Phenyl groups are generally attached to other atoms or groups. For example, triphenylmethane (Ph3 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Absolute Configuration
Absolute configuration refers to the spatial arrangement of atoms within a chiral molecular entity (or group) and its resultant stereochemical description. Absolute configuration is typically relevant in organic molecules, where carbon is bonded to four different substituents. This type of construction creates two possible enantiomers. Absolute configuration uses a set of rules to describe the relative positions of each bond around the chiral center atom. The most common labeling method uses the descriptors ''R'' or ''S'' is based on the Cahn–Ingold–Prelog priority rules. R and S refer to Rectus and Sinister, which are Latin for right and left, respectively. Chiral molecules can differ in their chemical properties, but are identical in their physical properties, which can make distinguishing enantiomers challenging. Absolute configurations for a chiral molecule (in pure form) are most often obtained by X-ray crystallography, although with some important limitations. All enant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Buprenorphine
Buprenorphine 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, it is typically started when withdrawal symptoms have begun and for the first two days of treatment 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. Maximum pain relief is generally within an hour with effects up to 24 hours. Buprenorphine affects different types of opioid receptors in different ways. Depending on the type of receptor, it may be an agonist, partial agonist, or antagonist. In the treatment of opioid use disorder buprenorphine is an agonist/antagonist, meaning that it relieves withdrawal symptoms from other opioids and induces some e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
