|
Salvinorin AB
Salvinorins are a group of natural chemical compounds and their structural analogs. Several salvinorins have been isolated from ''Salvia divinorum''. They are classified as diterpenoid furanolactones. Salvinorin A is a hallucinogen with dissociative effects. Several salvinorins have been isolated and characterized. Occurrence Originally isolated from ''S. divinorum'', salvinorins are also detected in smaller amounts in: * '' Salvia recognita'' (salvinorin A, 212.9 μg/g) * ''Salvia absconditiflora'' (salvinorin A at 51.5 μg/g, and salvinorin B at 402.2 μg/g) * ''Salvia glutinosa'' (salvinorin A, 38.9 μg/g) * '' Salvia potentillifolia'' (salvinorin B, 2352.0 μg/g) * '' Salvia adenocaulon'' (salvinorin B, 768.8 μg/g) For comparison, the amount of salvinorin A in ''S. divinorum'' ranges from 0.89 to 3.70 mg/g. All fractions reported are based on dry mass. Interestingly, the above reported species are not very closely related to ''S. divinorum''. Associated compounds I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Analog
A structural analog (analogue in modern traditional English; Commonwealth English), also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is screened for structural analogs of a lead compound. Chemical analogues of il ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salvia Glutinosa
''Salvia glutinosa'', the glutinous sage, sticky sage, Jupiter's sage, or Jupiter's distaff, is a herbaceous perennial plant belonging to the family Lamiaceae. Description ''Salvia glutinosa'' grows to approximately tall.Pignatti S. - Flora d'Italia – Edagricole – 1982. Vol. II, pag. 505 The stems are erect, with bright green hairy leaves that are about long, with petioles of about . The leaves are deciduous, toothed, pointed, tomentose and glandular. With the first frosts, foliage disappears and the plant is ready to overwinter in dormant buds. All parts of the plant are covered with sticky glandular hairs, especially the lime-green calyces and the flowers, resulting in the name "glutinosa". These sticky hairs probably have a protective function against predators. ''Salvia glutinosa'' is the main host plant of the plant bug ''Macrotylus quadrilineatus'', that feeds on the juices of the plant and on small insects entrapped on this sticky sage. Flowers grow in whorls of tw ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Functional Selectivity
Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid re ... [...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] |
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 |
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] |
Derivate
Derivatization is a technique used in chemistry which converts a chemical compound into a product (the reaction's derivate) of similar chemical structure, called a derivative. Generally, a specific functional group of the compound participates in the derivatization reaction and transforms the educt to a derivate of deviating reactivity, solubility, boiling point, melting point, aggregate state, or chemical composition. Resulting new chemical properties can be used for quantification or separation of the educt. Derivatization techniques are frequently employed in chemical analysis of mixtures and in surface analysis, e.g. in X-ray photoelectron spectroscopy where newly incorporated atoms label characteristic groups. Derivatization reactions Several characteristics are desirable for a derivatization reaction: # The reaction is reliable and proceeds to completion. Less unreacted starting material will simplify analysis. Also, this allows a small amount of analyte to be used. # T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 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] |
Salvinorin B Ethoxymethyl 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 A, salvinorin derivative and a κ- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
