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Decahydroisoquinoline
Decahydroisoquinoline is a nitrogen-containing heterocycle with the chemical formula . It is the saturated form of isoquinoline. Decahydroisoquinoline can be formed by the hydrogenation of isoquinoline or tetrahydroisoquinoline. Isomers There are four stereoisomers of decahydroisoquinoline which differ by the configuration of the two carbon atoms at the ring fusion: Occurrence The decahydroisoquinoline occurs naturally in some alkaloids, including gephyrotoxins and pumiliotoxin C which are found in amphibian skins. A variety of pharmaceutical drugs include a decahydroisoquinoline ring system within their structure, including ciprefadol, dasolampanel, nelfinavir, saquinavir, and tezampanel Tezampanel (, ) (developmental code names LY-293,558, LY-326,325, NGX-424) is a drug originally developed by Eli Lilly which acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with sel .... References {{reflist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tezampanel
Tezampanel (, ) (developmental code names LY-293,558, LY-326,325, NGX-424) is a drug originally developed by Eli Lilly which acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective and anticonvulsant properties, the former of which may, at least in part, occur via blockade of calcium uptake into neurons. Tezampanel has a range of effects which may be useful for medicinal purposes, as well as its applications in scientific research. It suppresses both the withdrawal symptoms from morphine and other opioids, and the development of tolerance, as well as having antihyperalgesic and analgesic effects in its own right. It also has anxiolytic effects in animal studies and has been suggested as a candidate for the treatment of anxiety Anxiety is an emotion characterised by an unpleasant state of inner wikt:turmoil, turmoil and incl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ciprefadol
Ciprefadol is an opioid analgesic that is an isoquinoline derivative most closely related to cyclazocine and picenadol, with a number of other related compounds known. Ciprefadol is a mixed agonist–antagonist In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, beh ... at μ-opioid receptors and can partly block the effects of morphine at low doses, though at higher doses it acts more like a full agonist. It is also a potent κ-opioid agonist, unlike the corresponding N-methyl and N-phenethyl derivatives which are reasonably μ-selective agonists. References Synthetic opioids Mu-opioid receptor agonists 3-Hydroxyphenyl compounds Decahydroisoquinolines Cyclopropyl compounds {{analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetrahydroisoquinoline
Tetrahydroisoquinoline (TIQ or THIQ), also known as AMPH-CR, is an organic compound with the chemical formula C9H11N. Classified as a secondary amine, it is derived from isoquinoline by hydrogenation. It is a colorless viscous liquid that is miscible with most organic solvents. The tetrahydroisoquinoline skeleton is encountered in a number of bioactive compounds and drugs. Pharmacology THIQ is a conformationally restrained (CR) or cyclized analogue of β-phenethylamine and amphetamine and is also known as AMPH-CR. In contrast to amphetamine however, THIQ fails to substitute for dextroamphetamine in rodent drug discrimination tests, suggesting that it lacks stimulant effects. Similar findings have been made for other tetrahydroisoquinoline analogues of psychoactive phenethylamines, for instance DOM-CR. In any case, THIQ does substitute for TDIQ (MDTIQ), a selective α2-adrenergic receptor ligand, indicating that it is not pharmacologically inactive. Reactions As a secon ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dasolampanel
Dasolampanel (INN, USAN, code name NGX-426) is an orally bioavailable analog of tezampanel and thereby competitive antagonist of the AMPA and kainate receptors which was under development by Raptor Pharmaceuticals/ Torrey Pines Therapeutics for the treatment of chronic pain conditions including neuropathic pain and migraine. It was developed as a follow-on compound to tezampanel, as tezampanel is not bioavailable orally and must be administered by intravenous injection Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutr ..., but ultimately neither drug was ever marketed. See also * Irampanel * Selurampanel References AMPA receptor antagonists Analgesics Antimigraine drugs Carboxylic acids Decahydroisoquinolines Kainate receptor antagonists Chlorobenzene derivatives ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nelfinavir
Nelfinavir, sold under the brand name Viracept, is an antiretroviral medication used in the treatment of HIV/AIDS. Nelfinavir belongs to the class of drugs known as protease inhibitor (pharmacology), protease inhibitors (PIs) and like other PIs is almost always used in combination with other antiretroviral drugs. Nelfinavir is an orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki = 2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection. It was patented in 1992 and approved for medical use in 1997. Toxicity Common (>1%) side effects include insulin resistance, hyperglycemia and lipodystrophy. Nelfinavir can produce a range of adverse side effects. Flatulence, diarrhea, or abdominal pain are common (i.e. experienced by more than one in one hundred patients). Fatigue, urination, rash, mouth ulcers, or hepatitis are less frequent effects (experienced by one in one thousand to one in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heterocycle
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic organic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of organic heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of organic heterocyclic chemistry focuses especially on organic unsaturated derivatives, and the preponderance of work and applications involves unstrained organic 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of organic heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Saturated And Unsaturated Compounds
A saturated compound is a chemical compound (or ion) that resists addition reactions, such as hydrogenation, oxidative addition, and the binding of a Lewis acids and bases, Lewis base. The term is used in many contexts and classes of chemical compounds. Overall, saturated compounds are less reactive than unsaturated compounds. Saturation is derived from the Latin word ''saturare'', meaning 'to fill'.An unsaturated compound is also a chemical compound (or ion) that attracts reduction reactions, such as dehydrogenation,oxidative reduction Organic chemistry Generally distinct types of unsaturated organic compounds are recognized. For hydrocarbons: *alkene (unsaturated) vs alkane (saturated) *alkyne (unsaturated) vs alkane (saturated) *arene (unsaturated) vs cycloalkane (saturated) For organic compounds containing heteroatoms (other than C and H), the list of unsaturated groups is long but some common types are: *carbonyl, e.g. ketones, aldehydes, esters, carboxylic acids (unsatura ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isoquinoline
Isoquinoline is an individual chemical specimen - a heterocyclic aromatic organic compound - as well as the name of a family of many thousands of natural plant alkaloids, any one of which might be referred to as "an isoquinoline". It is a structural isomer of quinoline. Isoquinoline and quinoline are benzopyridines, which are composed of a benzene ring fused to a pyridine ring. In a broader sense, the term isoquinoline is used to make reference to isoquinoline derivatives. 1-Benzylisoquinoline is the structural backbone in many naturally occurring alkaloids such as papaverine. The isoquinoline ring in these natural compound derives from the aromatic amino acid tyrosine. Properties Isoquinoline is a colorless hygroscopic liquid at temperatures above its melting point with a penetrating, unpleasant odor. Impure samples can appear brownish, as is typical for nitrogen heterocycles. It crystallizes in form of platelets that have a low solubility in water but dissolve well in et ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydrogenation
Hydrogenation is a chemical reaction between molecular hydrogen (H2) and another compound or element, usually in the presence of a catalyst such as nickel, palladium or platinum. The process is commonly employed to redox, reduce or Saturated and unsaturated compounds, saturate organic compounds. Hydrogenation typically constitutes the addition of pairs of hydrogen atoms to a molecule, often an alkene. Catalysts are required for the reaction to be usable; non-catalytic hydrogenation takes place only at very high temperatures. Hydrogenation reduces Double bond, double and Triple bond, triple bonds in hydrocarbons. Process Hydrogenation has three components, the Saturated and unsaturated compounds, unsaturated substrate, the hydrogen (or hydrogen source) and, invariably, a catalyst. The redox, reduction reaction is carried out at different temperatures and pressures depending upon the substrate and the activity of the catalyst. Related or competing reactions The same cataly ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stereoisomer
In stereochemistry, stereoisomerism, or spatial isomerism, is a form of isomerism in which molecules have the same molecular formula and sequence of bonded atoms (constitution), but differ in the three-dimensional orientations of their atoms in space. This contrasts with structural isomers, which share the same molecular formula, but the bond connections or their order differs. By definition, molecules that are stereoisomers of each other represent the same structural isomer. Enantiomers Enantiomers, also known as optical isomers, are two stereoisomers that are related to each other by a reflection: they are mirror images of each other that are non-superposable. Human hands are a macroscopic analog of this. Every stereogenic center in one has the opposite configuration in the other. Two compounds that are enantiomers of each other have the same physical properties, except for the direction in which they rotate polarized light and how they interact with different enantiomers of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alkaloid
Alkaloids are a broad class of natural product, naturally occurring organic compounds that contain at least one nitrogen atom. Some synthetic compounds of similar structure may also be termed alkaloids. Alkaloids are produced by a large variety of organisms including bacteria, fungus, fungi, Medicinal plant, plants, and animals. They can be purified from crude extracts of these organisms by acid-base extraction, or solvent extractions followed by silica-gel column chromatography. Alkaloids have a wide range of pharmacology, pharmacological activities including antimalarial medication, antimalarial (e.g. quinine), asthma, antiasthma (e.g. ephedrine), chemotherapy, anticancer (e.g. omacetaxine mepesuccinate, homoharringtonine), cholinomimetic (e.g. galantamine), vasodilation, vasodilatory (e.g. vincamine), Antiarrhythmic agent, antiarrhythmic (e.g. quinidine), analgesic (e.g. morphine), antibacterial (e.g. chelerythrine), and anti-diabetic, antihyperglycemic activities (e.g. berb ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gephyrotoxin
Gephyrotoxin is a naturally occurring product that stems from the Colombian tropical frog '' Dendrobates histrionicus''. It is a member of the class of compounds known as histrionicotoxins. This alkaloid skin secretion was first isolated from the tropical frog in 1977 by Daly and his fellow workers. Biological uses This compound is a relatively non-toxic chemical. At first it showed activity as a slight muscarinic antagonist, but with recent studies it has shown other interesting neurological activities. Due to these new activities, many laboratories want to conduct future research on it. Due to this demand and the scarcity and lack of abundance of the tree frog the synthesis of this product is of much interest. Synthesis The first total synthesis of gephyrotoxin was performed by Kishi and his co-workers, here they prepped an intermediate from L-pyroglutamic acid in 18 steps. Others have made it to the same intermediate in fewer steps but have included poorly diastereoselec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
