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Quadazocine
Quadazocine (WIN-44,441) is an opioid antagonist of the benzomorphan family which is used in scientific research. It acts as a silent antagonist at all three of the major opioid receptors— μ, κ, and δ, but with a significant preference in affinity for the μ receptor and the κ2 subtype. As such, it has been touted as a "κ2-selective" antagonist, though this is not entirely accurate on account of its similar affinity for the μ receptor. As would be expected, quadazocine reverses the effects (e.g., analgesia) of opioid agonists like morphine and fentanyl in animals. See also * Dezocine Dezocine, sold under the brand name Dalgan, is an atypical opioid analgesic which is used in the treatment of pain. It is used by intravenous infusion and intramuscular injection. Dezocine is an opioid receptor modulator, acting as a partial ... References Benzomorphans Cyclopentyl compounds Delta-opioid receptor antagonists Kappa-opioid receptor antagonists Mu-opioid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
κ-opioid Receptor
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind opioid-like compounds in the brain and are responsible for mediating the effects of these compounds. These effects include altering nociception, consciousness, motor control, and mood. Dysregulation of this receptor system has been implicated in alcohol and drug addiction. The KOR is a type of opioid receptor that binds the opioid peptide dynorphin as the primary endogenous ligand (substrate naturally occurring in the body). In addition to dynorphin, a variety of natural alkaloids, terpenes and synthetic ligands bind to the receptor. The KOR may provide a natural addiction control mechanism, and therefore, drugs that target this receptor may have therapeutic potential in the treatment of addiction. There is evidence that distribution ... [...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] |
Benzomorphan
Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma receptors, including the following compounds: * 5,9-DEHB * 8-CAC * Alazocine * Anazocine * Bremazocine * Butinazocine * Carbazocine * Cogazocine * Cyclazocine * Dezocine * Eptazocine * Etazocine * Ethylketocyclazocine * Fluorophen * Gemazocine * Ibazocine * Ketazocine * Metazocine * Moxazocine * Pentazocine * Phenazocine * Quadazocine * Thiazocine * Tonazocine * Volazocine * Zenazocine Some of these agents are used as analgesics, including pentazocine, phenazocine, dezocine, and eptazocine. See also * Benzazocine * Azocine * Morphinan Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative hallucinogens, among others. Structure Morphinan has a phenanthrene core stru ... References Benzomorphans {{organic-compou ... [...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 agonists, the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclopentyl Compounds
Cyclopentane (also called C pentane) is a highly flammable alicyclic hydrocarbon with chemical formula C5H10 and CAS number 287-92-3, consisting of a ring of five carbon atoms each bonded with two hydrogen atoms above and below the plane. It occurs as a colorless liquid with a petrol-like odor. Its melting point is −94 °C and its boiling point is 49 °C. Cyclopentane is in the class of cycloalkanes, being alkanes that have one or more rings of carbon atoms. It is formed by cracking cyclohexane in the presence of alumina at a high temperature and pressure. It was first prepared in 1893 by the German chemist Johannes Wislicenus. Production, occurrence and use Cycloalkanes are formed by catalytic reforming. For example, when passed over a hot platinum surfact, 2-methylbutane converts into cyclopentane. Cyclopentane has no particular use. No commercial products are made from cyclopentane itself. As a volatile hydrocarbon it is an incidental component of some fuels and b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dezocine
Dezocine, sold under the brand name Dalgan, is an atypical opioid analgesic which is used in the treatment of pain. It is used by intravenous infusion and intramuscular injection. Dezocine is an opioid receptor modulator, acting as a partial agonist of the μ- and κ-opioid receptors. It has a similar profile of effects to related opioids acting at the μ-opioid receptor, including analgesia and euphoria. Unlike other opioids acting at the κ-opioid receptor however, dezocine does not produce side effects such as dysphoria or hallucinations at any therapeutically used dose. Dezocine was first synthesized in 1970. It was introduced for medical use in the United States in 1986 but was not marketed in other countries. Dezocine was discontinued in the United States in 2011 with no official reason given. However, it has become one of the most widely used analgesics in China. In light of the opioid epidemic, dezocine has seen a resurgence in use and interest. Medical uses Dezoci ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fentanyl
Fentanyl, also spelled fentanil, is a very potent synthetic opioid used as a pain medication. Together with other drugs, fentanyl is used for anesthesia. It is also used illicitly as a recreational drug, sometimes mixed with heroin, cocaine, benzodiazepines or methamphetamine, among others. Its potentially deadly overdose effects can be neutralized by naloxone. Fentanyl is commonly used to create counterfeit pills disguised as OxyContin, Xanax, Adderall, among others. It has a rapid onset and its effects generally last under two hours. Medically, it is used by injection, nasal spray, or skin patch, or absorbed through the cheek as a lozenge or tablet. Common adverse effects of fentanyl include nausea, vomiting, constipation, itching, sedation, confusion, and injuries related to poor coordination. Serious adverse effects may include respiratory depression, hallucinations, serotonin syndrome, low blood pressure, or development of an opioid use disorder. Fentanyl works b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morphine
Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies (''Papaver somniferum''). It is mainly used as a analgesic, pain medication, and is also commonly used recreational drug, recreationally, or to make other illicit drug, illicit opioids. There are numerous methods used to administer morphine: oral; sublingual administration, sublingual; via inhalation; intramuscular, injection into a muscle; by Subcutaneous injection, injection under the skin; intravenously; Intrathecally, injection into the space around the spinal cord; 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 Ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesia
Pain management is an aspect of medicine and health care involving relief of pain (pain relief, analgesia, pain control) in various dimensions, from acute and simple to chronic and challenging. Most physicians and other health professionals provide some pain control in the normal course of their practice, and for the more complex instances of pain, they also call on additional help from a specific medical specialty devoted to pain, which is called pain medicine. Pain management often uses a multidisciplinary approach for easing the suffering and improving the quality of life of anyone experiencing pain, whether acute pain or chronic pain. Relief of pain in general (analgesia) is often an acute affair, whereas managing chronic pain requires additional dimensions. The typical pain management team includes medical practitioners, pharmacists, clinical psychologists, physiotherapists, occupational therapists, recreational therapists, physician assistants, nurses, and dentist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
