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Herkinorin
Herkinorin is an opioid analgesic that is an analog (chemistry), analogue of the natural product salvinorin A. It was discovered in 2005 during structure-activity relationship studies into neoclerodane diterpenes, the family of chemical compounds of which salvinorin A is a member. Unlike salvinorin A, which is a selective κ-opioid receptor agonist with no significant μ-opioid receptor affinity, herkinorin is predominantly a μ-opioid receptor agonist. Compared to salvinorin A, herkinorin has 47× lower Ligand_(biochemistry)#Receptor/ligand_binding_affinity, affinity for κ-opioid receptors (''K''i ＝ 90 nM vs ''K''i ＝ 1.9 nM), and at least 25× higher affinity for μ-opioid receptors (''K''i ＝ 12 nM vs ''K''i > 1000 nM), where it acts as a full agonist (IC50 ＝ 0.5 μM, Emax ＝ 130% vs DAMGO). Herkinorin is a semi-synthetic compound, made from salvinorin B, which is most conveniently made from salvinorin A by deacetylation, since, while both salvinorin A and salvinorin B ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salvinorin B
Salvinorin A is the main active psychotropic molecule in ''Salvia divinorum''. Salvinorin A is considered a dissociative hallucinogen. It is structurally distinct from other naturally occurring hallucinogens (such as DMT, psilocybin, and mescaline) because it contains no nitrogen atoms; hence, it is not an alkaloid (and cannot be rendered as a salt), but rather is a terpenoid. It also differs in subjective experience, compared to other hallucinogens, and has been described as dissociative. Salvinorin A can produce psychoactive experiences in humans with a typical duration of action being several minutes to an hour or so, depending on the method of ingestion. Salvinorin A is found with several other structurally related salvinorins. Salvinorin is a ''trans''-neoclerodane diterpenoid. It acts as a kappa opioid receptor agonist and is the first known compound acting on this receptor that is not an alkaloid. History Salvinorin A was first described and n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salvinorin A
Salvinorin A is the main active psychotropic molecule in '' Salvia divinorum''. Salvinorin A is considered a dissociative hallucinogen. It is structurally distinct from other naturally occurring hallucinogens (such as DMT, psilocybin, and mescaline) because it contains no nitrogen atoms; hence, it is not an alkaloid (and cannot be rendered as a salt), but rather is a terpenoid. It also differs in subjective experience, compared to other hallucinogens, and has been described as dissociative. Salvinorin A can produce psychoactive experiences in humans with a typical duration of action being several minutes to an hour or so, depending on the method of ingestion. Salvinorin A is found with several other structurally related salvinorins. Salvinorin is a ''trans''-neoclerodane diterpenoid. It acts as a kappa opioid receptor agonist and is the first known compound acting on this receptor that is not an alkaloid. History Salvinorin A was first described and named in 1982 ... [...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] |
Arrestin
Arrestins (abbreviated Arr) are a small family of proteins important for regulating signal transduction at G protein-coupled receptors. Arrestins were first discovered as a part of a conserved two-step mechanism for regulating the activity of G protein-coupled receptors (GPCRs) in the visual rhodopsin system by Hermann Kühn, Scott Hall, and Ursula Wilden and in the β-adrenergic system by Martin J. Lohse and co-workers. Function In response to a stimulus, GPCRs activate heterotrimeric G proteins. In order to turn off this response, or adapt to a persistent stimulus, active receptors need to be desensitized. The first step in desensitization is phosphorylation of the receptor by a class of serine/threonine kinases called G protein coupled receptor kinases (GRKs). GRK phosphorylation specifically prepares the activated receptor for arrestin binding. Arrestin binding to the receptor blocks further G protein-mediated signaling and targets receptors for internalization, and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Peripherally Selective Drugs
Periphery or peripheral may refer to: Music *Periphery (band), American progressive metal band * ''Periphery'' (album), released in 2010 by Periphery * "Periphery", a song from Fiona Apple's album '' The Idler Wheel...'' Gaming and entertainment *Periphery, a group of political entities in BattleTech, a wargaming franchise *''The Peripheral'', a 2014 novel by William Gibson **''The Peripheral'', a streaming series based on Gibson's novel Tech and math * Peripheral, an external device attached to a computer * Peripheral, an alternate mathematical term for boundary parallel in manifold theory *Peripheral cycle, a mathematical term in graph theory Political *Periphery countries, the least developed countries in world systems theory *Periphery (France), statistical area designating a commuter belt around an urban unit * Peripheries of Greece or ''administrative regions of Greece'' (Greek: , '), the country's first-level administrative divisions ** Peripheral units of Greec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Methyl Esters
In organic chemistry, a methyl group is an alkyl derived from methane, containing one carbon atom bonded to three hydrogen atoms, having chemical formula . In formulas, the group is often abbreviated as Me. This hydrocarbon group occurs in many organic compounds. It is a very stable group in most molecules. While the methyl group is usually part of a larger molecule, bounded to the rest of the molecule by a single covalent bond (), it can be found on its own in any of three forms: methanide anion (), methylium cation () or methyl radical (). The anion has eight valence electrons, the radical seven and the cation six. All three forms are highly reactive and rarely observed. Methyl cation, anion, and radical Methyl cation The methylium cation () exists in the gas phase, but is otherwise not encountered. Some compounds are considered to be sources of the cation, and this simplification is used pervasively in organic chemistry. For example, protonation of methanol gives an electr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzoate Esters
Benzoic acid is a white (or colorless) solid organic compound with the formula , whose structure consists of a benzene ring () with a carboxyl () substituent. It is the simplest aromatic carboxylic acid. The name is derived from gum benzoin, which was for a long time its only source. Benzoic acid occurs naturally in many plants and serves as an intermediate in the biosynthesis of many secondary metabolites. Salts of benzoic acid are used as food preservatives. Benzoic acid is an important precursor for the industrial synthesis of many other organic substances. The salts and esters of benzoic acid are known as benzoates . History Benzoic acid was discovered in the sixteenth century. The dry distillation of gum benzoin was first described by Nostradamus (1556), and then by Alexius Pedemontanus (1560) and Blaise de Vigenère (1596). Justus von Liebig and Friedrich Wöhler determined the composition of benzoic acid. These latter also investigated how hippuric acid is related ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RB-64
RB-64 (22-thiocyanatosalvinorin A) is a semi-synthetic salvinorin A, salvinorin derivative and a κ-opioid receptor (KOR) agonist which is used in scientific research. Its most remarkable property is its functional selectivity for G protein versus Arrestin beta 2, β-arrestin-2. RB-64 has a functional selectivity#bias factor, bias factor of 96 and is analgesic with fewer of the side-effects associated with unbiased KOR agonists. The analgesia-like effect is long-lasting. Compared with unbiased agonists, RB-64 evokes considerably less Receptor-mediated endocytosis, receptor internalization. See also * Herkinorin * Salvinorin B methoxymethyl ether * Salvinorin A * Nalfurafine References Further reading * * Synthetic opioids Kappa-opioid receptor agonists Kappa-opioid receptor antagonists Thiocyanates Biased ligands {{Organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salvinorin B Methoxymethyl Ether
Salvinorin B methoxymethyl ether (2-''O''-methoxymethylsalvinorin B) is a semi-synthetic analogue of the natural product salvinorin A used in scientific research. It has a longer duration of action of around 2–3 hours, compared to less than 30 minutes for salvinorin A, and has increased affinity and potency at the κ-opioid receptor. It is made from salvinorin B, which is most conveniently made from salvinorin A by deacetylation. The crystal structure reveals that the methoxy group overlaps with the acetyl group of salvinorin A, but with a different orientation. Salvinorin B methoxymethyl ether has a Ki of 0.60 nM at the κ opioid receptor, and is around five times more potent than salvinorin A in animal studies, although it is still only half as potent as its stronger homolog salvinorin B ethoxymethyl ether (symmetry). See also * Salvinorin B ethoxymethyl ether * RB-64 RB-64 (22-thiocyanatosalvinorin A) is a semi-synthetic salvinorin derivative and a κ-opioid rece ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kurkinorin
Kurkinorin is a non-nitrogenous, extremely selective centrally acting μ-opioid receptor agonist derived from salvinorin A with no sedating or rewarding effects. See also * Herkinorin * Samidorphan * 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- ... References {{Reflist Heterocyclic compounds with 3 rings Isochromenes 3-Furyl compounds Methyl esters Benzoate esters ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
