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5'-Guanidinonaltrindole
5'-Guanidinonaltrindole (5'-GNTI) is an opioid antagonist used in scientific research which is highly selective for the κ opioid receptor. It is 5x more potent and 500 times more selective than the commonly used κ-opioid antagonist norbinaltorphimine. It has a slow onset and long duration of action, and produces antidepressant effects in animal studies. It also increases allodynia by interfering with the action of the κ-opioid peptide dynorphin. In addition to activity at the KOR, 5'-GNTI has been found to act as a positive allosteric modulator of the α1A-adrenergic receptor ( EC50 = 41 nM), and this may contribute to its "severe transient effects". See also * 6'-Guanidinonaltrindole * Binaltorphimine * JDTic JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the ... Ref ... [...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] |
Semisynthetic Opioids
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] |
6'-Guanidinonaltrindole
6′-Guanidinonaltrindole (6′-GNTI) is a κ– δ- opioid receptor selective ligand used in scientific research. With 6′-GNTI, evidence was provided for the first time that receptor oligomerization plays functional role in living organisms. 6′-GNTI is an extremely biased agonist of the κ-opioid receptor. It is a potent partial agonist of the G protein pathway but does not recruit the β-arrestin pathway. Due to its functional selectivity for the G protein pathway, 6′-GNTI functions as an antagonist of nonbiased KOR agonists on the β-arrestin pathway. It is thought that 6′-GTNI may be able to produce analgesia without dysphoria and with a lower incidence of tolerance. See also * 5′-Guanidinonaltrindole * RB-64 * Noribogaine * ICI-199,441 ICI-199,441 is a drug which acts as a potent and selective κ-opioid agonist, and has analgesic effects. It is a biased agonist of the KOR, and is one of a relatively few KOR ligands that is G protein-biased rather than ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binaltorphimine
Binaltorphimine (BNI) is a selective antagonist of the κ-opioid receptor (KOR). BNI and norbinaltorphimine (nor-BNI) were the first highly selective KOR antagonists to be discovered. See also * 5'-GNTI * JDTic JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the ... References 4,5-Epoxymorphinans Phenols Tertiary alcohols Kappa-opioid receptor antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norbinaltorphimine
Norbinaltorphimine (nor-BNI or nBNI) is an opioid antagonist used in scientific research. It is one of the few opioid antagonists available that is highly selective for the κ-opioid receptor, and blocks this receptor without affecting the μ- or 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 lig ...s, although it has less selectivity ''in vivo'' than when used in isolated tissues. nor-BNI blocks the effects of κ-opioid agonists in animal models, and produces antidepressant and antipanic-like effects. See also * Binaltorphimine * 5'-Guanidinonaltrindole * JDTic References 4,5-Epoxymorphinans Irreversible antagonists Phenols Tertiary alcohols Kappa-opioid receptor antagonists {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with formald ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Irreversible Antagonists ''
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Irreversible may refer to: *Irreversible process, in thermodynamics, a process that is not reversible *''Irréversible'', a 2002 film * ''Irréversible'' (soundtrack), soundtrack to the film ''Irréversible'' * An album recorded by hip-hop artist Grieves * A song by progressive metalcore band Erra from their 2016 album ''Drift Drift or Drifts may refer to: Geography * Drift or ford (crossing) of a river * Drift, Kentucky, unincorporated community in the United States * In Cornwall, England: ** Drift, Cornwall, village ** Drift Reservoir, associated with the village ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Guanidines
Guanidine is the compound with the formula HNC(NH2)2. It is a colourless solid that dissolves in polar solvents. It is a strong base that is used in the production of plastics and explosives. It is found in urine predominantly in patients experiencing renal failure. A guanidine moiety also appears in larger organic molecules, including on the side chain of arginine. Structure Guanidine can be thought of as a nitrogenous analogue of carbonic acid. That is, the C=O group in carbonic acid is replaced by a C=NH group, and each OH is replaced by a group. Isobutene can be seen as the carbon analogue in much the same way. A detailed crystallographic analysis of guanidine was elucidated 148 years after its first synthesis, despite the simplicity of the molecule. In 2013, the positions of the hydrogen atoms and their displacement parameters were accurately determined using single-crystal neutron diffraction. Production Guanidine can be obtained from natural sources, being first isolat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-1 Adrenergic Receptor Agonists
{{disambiguation ...
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency, a genetic disorder *Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in '' Buzz Lightyear of Star Command: The Adventure Begins'' * ''Alpha 1'' (Robert Silverberg anthology), a 1970 book See also * * *Alpha (other) *AMY1A or Alpha-1A or, an enzyme found in humans and other mammals *List of A1 genes, proteins or receptors This is a list of genes, proteins or receptors named A1 or Alpha-1 : * Actin, alpha 1 * Actinin, alpha 1 * Adaptor-related protein complex 2, alpha 1 * Aldehyde dehydrogenase 3 family, member A1 * Aldehyde dehydrogenase 4 family, member A1 * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JDTic
JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the MOR antagonist alvimopan. In addition, it is structurally distinct from other KOR antagonists such as norbinaltorphimine. JDTic has been used to create crystal structures of KOR Pharmacology JDTic is a long-acting ("inactivating") antagonist of the KOR, and is reported to be highly selective for the KOR over the μ-opioid receptor (MOR), δ-opioid receptor (DOR), and nociceptin receptor (NOP). However, in another study, JDTic showed little selectivity over the μ-opioid receptor, though it failed to block the effects of the selective μ-opioid receptor agonist sufentanil across a wide range of doses in animals. It has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
