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δ-Opioid Receptor
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous ligands. The regions of the brain where the δ-opioid receptor is largely expressed vary from species model to species model. In humans, the δ-opioid receptor is most heavily expressed in the basal ganglia and neocortical regions of the brain. Function The endogenous system of opioid receptors is well known for its analgesic potential; however, the exact role of δ-opioid receptor activation in pain modulation is largely up for debate. This also depends on the model at hand since receptor activity is known to change from species to species. Activation of delta receptors produces analgesia, perhaps as significant potentiators of μ-opioid receptor agonists. However, it seems like delta agonism provides heavy potentiation to any mu agonism. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid Receptor
Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin receptors (SSTRs). Opioid receptors are distributed widely in the brain, in the spinal cord, on peripheral neurons, and digestive tract. Discovery By the mid-1960s, it had become apparent from pharmacologic studies that opiate drugs were likely to exert their actions at specific receptor sites, and that there were likely to be multiple such sites. Early studies had indicated that opiates appeared to accumulate in the brain. The receptors were first identified as specific molecules through the use of binding studies, in which opiates that had been labeled with radioisotopes were found to bind to brain membrane homogenates. The first such study was published in 1971, using 3H-levorphanol. In 1973, Candace Pert and Solomon H. Snyder publis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Animal Models Of Depression
Animal models of depression are research tools used to investigate depression and action of antidepressants as a simulation to investigate the symptomatology and pathophysiology of depressive illness or used to screen novel antidepressants. Introduction Depression Major depressive disorder, also called "clinical depression" or often simply "depression", is a common, long-lasting and diverse psychiatric syndrome that significantly affects a person's thoughts, behavior, feelings and sense of well-being. Symptoms include low mood and aversion to activity. Depressed people may also feel sad, anxious, empty, hopeless, worried, helpless, worthless, guilty, irritable, hurt, or restless. They may lose interest in activities that once were pleasurable, experience loss of appetite or overeating, have problems concentrating, remembering details, or making decisions, and may contemplate or attempt suicide. Insomnia, excessive sleeping, fatigue, loss of energy, or aches, pains, or digesti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Delta Ligands
Delta commonly refers to: * Delta (letter) (Δ or δ), a letter of the Greek alphabet * River delta, at a river mouth * D (NATO phonetic alphabet: "Delta") * Delta Air Lines, US * Delta variant of SARS-CoV-2 that causes COVID-19 Delta may also refer to: Places Canada * Delta, British Columbia ** Delta (electoral district), a federal electoral district ** Delta (provincial electoral district) * Delta, Ontario United States * Mississippi Delta * Delta, Alabama * Delta Junction, Alaska * Delta, Colorado * Delta, Illinois * Delta, Iowa * Delta, Kentucky * Delta, Louisiana * Delta, Missouri * Delta, North Carolina * Delta, Ohio * Delta, Pennsylvania * Sacramento–San Joaquin River Delta, California * Delta, Utah * Delta, Wisconsin, a town * Delta (community), Wisconsin * Delta County (other) Elsewhere * Delta Island, Antarctica * Delta Stream, Antarctica * Delta, Minas Gerais, Brazil * Nile Delta, Egypt * Delta, Thessaloniki, Greece * Delta State, Nigeria * Delta, Astr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Delta Opioid Ligands
Delta commonly refers to: * Delta (letter) (Δ or δ), a letter of the Greek alphabet * River delta, at a river mouth * D (NATO phonetic alphabet: "Delta") * Delta Air Lines, US * Delta variant of SARS-CoV-2 that causes COVID-19 Delta may also refer to: Places Canada * Delta, British Columbia ** Delta (electoral district), a federal electoral district ** Delta (provincial electoral district) * Delta, Ontario United States * Mississippi Delta * Delta, Alabama * Delta Junction, Alaska * Delta, Colorado * Delta, Illinois * Delta, Iowa * Delta, Kentucky * Delta, Louisiana * Delta, Missouri * Delta, North Carolina * Delta, Ohio * Delta, Pennsylvania * Sacramento–San Joaquin River Delta, California * Delta, Utah * Delta, Wisconsin, a town * Delta (community), Wisconsin * Delta County (other) Elsewhere * Delta Island, Antarctica * Delta Stream, Antarctica * Delta, Minas Gerais, Brazil * Nile Delta, Egypt * Delta, Thessaloniki, Greece * Delta State, Nigeria * Delta, Astr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naltrindole
Naltrindole is a highly potent, highly selective delta opioid receptor antagonist used in biomedical research. In May 2012 a paper was published in ''Nature'' with the structure of naltrindole in complex with the mouse δ-opioid G-protein coupled receptor, solved by X-ray crystallography. Drug design Since peptide compounds are unable to cross the blood–brain barrier, researchers developed naltrindole to be a non-peptide antagonist analog of the delta-preferring endogenous opiate enkephalin. Enkephalin contains an aromatic phenyl group on its Phe4 residue, which was hypothesized to be the "address" sequence responsible for the opiate's delta opioid receptor affinity. Thus, attachment of a phenyl-containing indole molecule to the C-ring of naltrexone's 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DPI-3290
DPI-3290 was discovered by scientists at Burroughs Wellcome and licensed to Delta Pharmaceutical and is a drug that is used in scientific research. It is a potent analgesic drug, which produces little respiratory depression. DPI-3290 acts as an agonist at both μ- and δ-opioid receptor, with an IC50 of 6.2nM at μ and 1.0nM at δ. See also * BW373U86 * DPI-221 * DPI-287 DPI-287 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces less convulsions than most drugs from this family. It has antidepressant Antidepressants are a class ... References {{Piperazines Synthetic opioids Delta-opioid receptor agonists Piperazines Benzanilides Phenols Fluoroarenes Allyl compounds Mu-opioid receptor agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DPI-287
DPI-287 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces less convulsions than most drugs from this family. It has antidepressant Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, hea ...-like effects. References Synthetic opioids Delta-opioid receptor agonists Benzamides Piperazines Phenols {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BW373U86
(+)-BW373U86 is an opioid analgesic drug used in scientific research. BW373U86 is a selective agonist for the δ-opioid receptor, with approximately 15x stronger affinity for the δ-opioid than the μ-opioid receptor. It has potent analgesic and antidepressant effects in animal studies. In studies on rats, BW373U86 appears to protect heart muscle cells from apoptosis in conditions of ischemia Ischemia or ischaemia is a restriction in blood supply to any tissue, muscle group, or organ of the body, causing a shortage of oxygen that is needed for cellular metabolism (to keep tissue alive). Ischemia is generally caused by problems wi ... (oxygen deprivation, such as in heart attack). The mechanism for this is complex and may be separate from its delta agonist effects. References {{DEFAULTSORT:Bw373u86 Synthetic opioids Respiratory agents Delta-opioid receptor agonists Phenols Benzamides Piperazines Allyl compounds Mu-opioid receptor agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SNC-80
SNC-80 is an opioid analgesic compound that selectively activates μ–δ opioid receptor heteromers and is used in scientific research. It was discovered in 1994. SNC-80 was the first non-peptide compound developed that was regarded as a highly selective agonist for the δ-opioid receptor. It has been shown to produce useful analgesic, antidepressant and anxiolytic effects in animal studies, but its usefulness is limited by producing convulsions 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 sometimes used as a s ... at high doses, and so SNC-80 is not used medically, although it is a useful compound in scientific research. References Opioids Delta-opioid receptor agonists Benzamides Piperazines Phenol ethers Allyl compounds Receptor heteromer ligands {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Deltorphin
Deltorphin, also known as deltorphin A and dermenkephalin, is a naturally occurring, exogenous opioid heptapeptide and thus, exorphin, with the amino acid sequence Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2. Along with the other deltorphins (such as deltorphin I and deltorphin II) and the dermorphins, deltorphin is endogenous to frogs of the genus ''Phyllomedusa'' such as '' P. bicolor'' and '' P. sauvagei'' where it is produced in their skin, and is not known to occur naturally in any other species. Deltorphin is one of the highest affinity and most selective naturally occurring opioid peptides known, acting as a very potent and highly specific agonist of the δ-opioid receptor. Deltorphins have an unusually high blood–brain barrier penetration rate. The nonselective opiate antagonist naloxone inhibits deltorphin uptake by brain microvessels, but neither the selective δ-opioid antagonist naltrindole nor a number of opioid peptides with different affinities for δ- or μ-opioid rece ... [...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] |
Opiate
An opiate, in classical pharmacology, is a substance derived from opium. In more modern usage, the term ''opioid'' is used to designate all substances, both natural and synthetic, that bind to opioid receptors in the brain (including antagonists). Opiates are alkaloid compounds naturally found in the opium poppy plant ''Papaver somniferum''. The psychoactive compounds found in the opium plant include morphine, codeine, and thebaine. Opiates have long been used for a variety of medical conditions with evidence of opiate trade and use for pain relief as early as the eighth century AD. Opiates are considered drugs with moderate to high abuse potential and are listed on various "Substance-Control Schedules" under the Uniform Controlled Substances Act of the United States of America. In 2014, between 13 and 20 million people used opiates recreationally (0.3% to 0.4% of the global population between the ages of 15 and 65). According to the CDC, from this population, there were 47,00 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
