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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 alpha subunit, 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 Neocortex, 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 poten ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
G-protein Coupled Receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large protein family, group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell (biology), cell and activate cellular responses. They are coupled with G proteins. They pass through the cell membrane seven times in the form of six loops (three extracellular loops interacting with ligand molecules, three intracellular loops interacting with G proteins, an N-terminus, N-terminal extracellular region and a C-terminal intracellular region) of amino acid residues, which is why they are sometimes referred to as seven-transmembrane receptors. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) licence/ref> Ligands can bind either to the extracellular N-terminus and loops (e.g. glutama ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Animal Models Of Depression
Animal models of depression are research tools used to investigate Major depressive disorder, depression and action of antidepressant, antidepressants. They are used as a simulation to investigate the symptomatology and pathophysiology of depressive illness and to screen novel antidepressants. These models provide insights into molecular, genetic, and epigenetic factors associated with depression. Criteria for valid animal models include face, construct, and predictive validity. Endophenotypes, such as anhedonia, Behavioural despair test, behavioral despair, changes in appetite, neuroanatomical alterations, neuroendocrine disturbances, alterations in sleep architecture, and anxiety-related behaviors, are evaluated in these models. Antidepressant screening tests are employed to assess the effects of genetic, pharmacological, or environmental manipulations. Stress models including learned Learned helplessness, helplessness, chronic mild stress, and Social defeat, social defeat stress ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Delta Ligands
Delta commonly refers to: * Delta (letter) (Δ or δ), the fourth letter of the Greek alphabet * D (NATO phonetic alphabet: "Delta"), the fourth letter in the Latin alphabet * River delta, at a river mouth * Delta Air Lines, a major US carrier Delta may also refer to: Places Canada * Delta, British Columbia ** Delta (federal electoral district), a federal electoral district ** Delta (provincial electoral district) * Delta, Ontario United States * Mississippi Delta * Arkansas 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 and an unincorporated community * Delta County (other) Elsewhere * Delta Island, Antarctica * Delta Stream, Antarctica * Delta, Minas Gerais, Brazil * Nile Delta, Egypt * Delta, Thessalon ... [...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. Typical examples includ ... [...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 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 alpha subunit, Gi/G0 and has enkephalins as it ..., with an IC50 of 6.2nM at μ and 1.0nM at δ. See also * AZD2327 * BW373U86 * DPI-221 * DPI-287 References {{Piperazines Synthetic opioids Delta-opioid receptor agonists Piperazines Benzanilides 3-Hydroxyphenyl compounds 3-Fluorophenyl compounds 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-like effects. See also * AZD2327 * BW373U86 * 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 a ... References Synthetic opioids Delta-opioid receptor agonists Benzamides Piperazines 3-Hydroxyphenyl compounds Diethylamino compounds {{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 15× 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 (oxygen deprivation, such as in heart attack). The mechanism for this is complex and may be separate from its delta agonist effects. CNS review: See also * AZD2327 * DPI-287 * 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 a ... References {{DEFAULTSORT:Bw373u86 Synthetic opioids Respiratory agents Delta-opioid receptor agonists 3-Hydroxyphenyl compounds Benzamides Pi ... [...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 primarily in scientific research. Discovered in 1994, SNC-80 was a pioneering non-peptide compound regarded as a highly selective agonist for the δ-opioid receptor. 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 often used as a synony ... 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 Benz ... [...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 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 alpha subunit, Gi/G0 and has enkephalins as it .... Deltorphins have an unusually high blood–brain ba ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Opioid
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] |
Opiate
An opiate is an alkaloid substance derived from opium (or poppy straw). It differs from the similar term ''opioid'' in that the latter 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. Most 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 opioids recreationally, representing 0.3% to 0.4% of the global population between the ages of 15 and 65. According to the CDC, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
