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Lysergine
Lysergine, also known as 9,10-didehydro-6,8β-dimethylergoline, is an ergot alkaloid and serotonin receptor agonist of the ergoline family. It is a minor constituent of ergot. Pharmacology Lysergine shows selectivity for activation of the serotonin 5-HT2A receptor over several other closely related serotonin receptors (54-fold over the 5-HT2B receptor, 38-fold over the 5-HT2C receptor, and 127-fold over the 5-HT1A receptor). The drug is a partial agonist of the 5-HT2A receptor with moderate intrinsic activity (Emax = 57%). An analogue of lysergine, (+)-13-fluorolysergol, is an even more selective agonist of the 5-HT2A receptor than lysergine (EC50 for 5-HT2B and 5-HT2C of >10,000nM). However, this compound has relatively weak maximal efficacy in activating the receptor (Emax = 17%). See also * Descarboxylysergic acid * Lysergic acid * Ergine * Lysergol * SDZ SER-082 SER-082, or SDZ SER-082, is a binding selectivity, selective serotonin 5-HT2B receptor, 5-HT2B and 5 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SDZ SER-082
SER-082, or SDZ SER-082, is a binding selectivity, selective serotonin 5-HT2B receptor, 5-HT2B and 5-HT2C receptor, 5-HT2C receptor receptor antagonist, antagonist or weak partial agonist with an ergoline-like chemical structure, structure which is used in scientific research. It shows similar affinity (pharmacology), affinity for the serotonin 5-HT2B and 5-HT2C receptors and has ~40-fold higher affinity for the serotonin 5-HT2C receptor over the closely related serotonin 5-HT2A receptor, 5-HT2A receptor. Usages It has been used in animal studies into the behavioural effects of the different 5-HT2 subtypes, and how they influence the effects of other drugs such as cocaine. The drug has been found to have no effect on anxiety in multiple paradigms in rodents. In contrast to other serotonin 5-HT2C receptor antagonists, SER-082 does not produce hyperlocomotion in rodents, and instead can produce hypolocomotion at high doses that is independent of the serotonin 5-HT2C receptor. It ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lysergol
Lysergol is an alkaloid of the ergoline family that occurs as a minor constituent in some species of fungi (most within ''Claviceps''), and in the morning glory family of plants (Convolvulaceae), including the hallucinogenic seeds of '' Rivea corymbosa'' (ololiuhqui), '' Argyreia nervosa'' (Hawaiian baby woodrose) and '' Ipomoea violacea''. Lysergol can be synthesised using a tandem reaction to construct the piperidine skeleton and a rhodium-catalyzed + 2annulation in the late-stage indole formation. The binding of lysergol, as well as of isolysergol, to the serotonin 5-HT1A, 5-HT2A, 5-HT2B, and 5-HT2C receptors has been described. In contrast to LSD and other lysergamides, lysergol is non-hallucinogenic in humans and is described as not contributing to the hallucinogenic effects of morning glory seeds. It was inactive as a hallucinogen at doses of 2 to 8mg orally, up to more than 100times the effective dosage of LSD, but did produce light sedative-like effects at the 8m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Receptor
The 5-HT2A receptor is a subtype of the 5-HT2 receptor, 5-HT2 receptor that belongs to the serotonin receptor family and functions as a GPCR, G protein-coupled receptor (GPCR). It is a cell surface receptor that activates multiple intracellular signalling cascades. Like all 5-HT2 receptors, the 5-HT2A receptor is coupled to the Gq protein, Gq/G11 signaling pathway. It is the primary excitatory receptor subtype among the serotonin-responsive GPCRs. The 5-HT2A receptor was initially noted for its central role as the primary target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. It later regained research prominence when found to mediate, at least in part, the effects of many antipsychotic drugs, particularly atypical antipsychotic, atypical antipsychotics. Downregulation of post-synaptic 5-HT2A receptors is an adaptive response triggered by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Elevated 5-HT2A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Descarboxylysergic Acid
Descarboxylysergic acid, or 8-descarboxylysergic acid, also known as 9,10-didehydro-6-methylergoline or as 6-methyl-9-ergolene, is a drug of the ergoline family related to lysergic acid and lysergamides like lysergic acid diethylamide (LSD). It is the analogue of lysergic acid in which the carboxyl group at the C8 position of the molecule has been removed. Descarboxylysergic acid was synthesized in an attempt to help elucidate the minimum structural requirements for biological activity of ergoline and lysergamide drugs like LSD. Pharmacology In contrast to lysergic acid, which is said to have "very unexceptional biological activity", descarboxylysergic acid was, surprisingly, found to produce effects in mice that were described as remarkably similar to those of LSD. However, it was said that the specific tests performed were not reliably indicative of hallucinogenic effects in humans. Moreover, no other assays of hallucinogen-type effects were carried out, and descarboxylysergi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ergot Alkaloid
Ergoline is a core structure in many alkaloids and their synthetic derivatives. Ergoline alkaloids were first characterized in ergot. Some of these are implicated in the condition of ergotism, which can take a convulsive form or a gangrenous form. Even so, many ergoline alkaloids have been found to be clinically useful. Annual world production of ergot alkaloids has been estimated at 5,000–8,000 kg of all ergopeptines and 10,000–15,000 kg of lysergic acid, used primarily in the manufacture of semi-synthetic derivatives. Others, such as lysergic acid diethylamide, better known as LSD, a Semisynthesis, semi-synthetic derivative, and ergine, a natural derivative found in ''Argyreia nervosa'', ''Ipomoea tricolor'' and related species, are known Psychedelic drug, psychedelic substances. Natural occurrence Ergoline alkaloids are found in fungi such as Claviceps purpurea, Claviceps paspali, and the related Periglandula, which have a permanent, symbiotic bond with numerous ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nanomolar
Molar concentration (also called molarity, amount concentration or substance concentration) is the number of moles of solute per liter of solution. Specifically, It is a measure of the concentration of a chemical species, in particular, of a solute in a solution, in terms of amount of substance per unit volume of solution. In chemistry, the most commonly used unit for molarity is the number of moles per liter, having the unit symbol mol/L or mol/ dm3 (1000 mol/ m3) in SI units. A solution with a concentration of 1 mol/L is said to be 1 molar, commonly designated as 1 M or 1 M. Molarity is often depicted with square brackets around the substance of interest; for example, the molarity of the hydrogen ion is depicted as + Definition Molar concentration or molarity is most commonly expressed in units of moles of solute per litre of solution. For use in broader applications, it is defined as amount of substance of solute per unit volume of solution, or ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ergot Alkaloids
Ergot ( ) or ergot fungi refers to a group of fungus, fungi of the genus ''Claviceps''. The most prominent member of this group is ''Claviceps purpurea'' ("rye ergot fungus"). This fungus grows on rye and related plants, and produces alkaloids that can cause ergotism in humans and other mammals who consume grains contaminated with its fruiting structure (called ''ergot sclerotium''). ''Claviceps'' includes about 50 known species, mostly in the tropical regions. Economically significant species include ''C. purpurea'' (parasitic on Poaceae, grasses and cereals), ''C. fusiformis'' (on pearl millet, buffel grass), ''C. paspali'' (on dallis grass), ''C. africana'' (on sorghum) and ''C. lutea'' (on paspalum). ''C. purpurea'' most commonly affects Open pollination, outcrossing species such as rye (its most common host), as well as triticale, wheat and barley. It affects oats only rarely. ''C. purpurea'' has at least three races or varieties, which differ in their host specificity: *G ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ergolines
Ergoline is a core structure in many alkaloids and their synthetic derivatives. Ergoline alkaloids were first characterized in ergot. Some of these are implicated in the condition of ergotism, which can take a convulsive form or a gangrenous form. Even so, many ergoline alkaloids have been found to be clinically useful. Annual world production of ergot alkaloids has been estimated at 5,000–8,000 kg of all ergopeptines and 10,000–15,000 kg of lysergic acid, used primarily in the manufacture of semi-synthetic derivatives. Others, such as lysergic acid diethylamide, better known as LSD, a semi-synthetic derivative, and ergine, a natural derivative found in ''Argyreia nervosa'', ''Ipomoea tricolor'' and related species, are known psychedelic substances. Natural occurrence Ergoline alkaloids are found in fungi such as Claviceps purpurea, Claviceps paspali, and the related Periglandula, which have a permanent, symbiotic bond with numerous flowering vines, most notably, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ergine
Ergine, also known as lysergic acid amide (LSA or LAA) as well as LA-111, is a psychoactive compound of the ergoline and lysergamide families related to lysergic acid diethylamide (LSD). Ergine is an ergoline alkaloid found in fungi such as '' Claviceps paspali'' (ergot) and '' Periglandula'' species such as '' Periglandula clandestina'', which are permanently connected with many morning glory vines. Ergine induces relatively mild psychedelic effects as well as pronounced sedative effects. The most common sources of ergine for use as a drug are the seeds of morning glory species including ''Ipomoea tricolor'' (tlitliltzin), '' Ipomoea corymbosa'' (ololiuhqui), and '' Argyreia nervosa'' (Hawaiian baby woodrose). Morning glory seeds have a history of entheogenic use in Mesoamerica dating back at least hundreds of years. They have also since been used by many Westerners. In addition to ergine, morning glory seeds contain other ergolines such as lysergic acid hydroxyethylamid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lysergic Acid
Lysergic acid, also known as -lysergic acid and (+)-lysergic acid, is a precursor for a wide range of ergoline alkaloids that are produced by the ergot fungus and found in the seeds of '' Argyreia nervosa'' ( Hawaiian baby woodrose), and ''Ipomoea'' species ( morning glories, ololiuhqui, tlitliltzin). Amides of lysergic acid, lysergamides, are widely used as pharmaceuticals and as psychedelic drugs, e.g. lysergic acid diethylamide (LSD). Lysergic acid is listed as a Table I precursor under the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. The name Lysergic acid comes from the fact that it is a carboxylic acid, and it was first made by hydrolysis of various ergot alkaloids. Synthesis Laboratory Lysergic acid is generally produced by hydrolysis of natural lysergamides, but can also be synthesized in the laboratory by a complex total synthesis, for example by Robert Burns Woodward's team in 1956. An enantioselective total ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, 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 isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), 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 virtual screening, screened for structural analogs of a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
