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Vedaclidine
Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes. It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief. Synthesis : The Knoevenagel condensation between 3-Quinuclidone 731-38-2(1) & ethyl cyanoacetate 05-56-6(2) gives Ethyl (1-azabicyclo .2.2ctan-3-ylidine)cyanoacetateCID:54445383(3). The catalytic hydrogenation of the olefin group gave Ethyl (1-azabicyclo .2.2ctan-3-yl)cyanoacetate 41593-50-2(4). The reac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vedaclidine Synthesis
Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes. It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief. Synthesis : The Knoevenagel condensation between 3-Quinuclidone 731-38-2(1) & ethyl cyanoacetate 05-56-6(2) gives Ethyl (1-azabicyclo .2.2ctan-3-ylidine)cyanoacetateCID:54445383(3). The catalytic hydrogenation of the olefin group gave Ethyl (1-azabicyclo .2.2ctan-3-yl)cyanoacetate 41593-50-2(4). The reaction wit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Talsaclidine
Talsaclidine (WAL-2014) is a non- selective muscarinic acetylcholine receptor agonist which acts as a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes. It was under development for the treatment of Alzheimer's disease but showed only modest or poor efficacy in rhesus monkeys and humans, respectively, perhaps due to an array of dose-limiting side effects including increased heart rate and blood pressure, increased salivation, urinary frequency and burning upon urination, increased lacrimation and nasal secretion, abnormal accommodation, heartburn, upset stomach as well as cramps, nausea, vomiting and diarrhea, excessive sweating and palpitations. See also * Aceclidine * Vedaclidine Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an ... Referenc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Agonists
A muscarinic agonist is an agent that activates the activity of the muscarinic acetylcholine receptor. The muscarinic receptor has different subtypes, labelled M1-M5, allowing for further differentiation. Clinical significance M1 M1-type muscarinic acetylcholine receptors play a role in cognitive processing. In Alzheimer disease (AD), amyloid formation may decrease the ability of these receptors to transmit signals, leading to decreased cholinergic activity. As these receptors themselves appear relatively unchanged in the disease process, they have become a potential therapeutic target when trying to improve cognitive function in patients with AD. A number of muscarinic agonists have been developed and are under investigation to treat AD. These agents show promise as they are neurotrophic, decrease amyloid depositions, and improve damage due to oxidative stress. Tau-phosphorylation is decreased and cholinergic function enhanced. Notably several agents of the AF series of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aceclidine
Aceclidine (Glaucostat, Glaunorm, Glaudin) is a parasympathomimetic miotic agent used in the treatment of narrow angle glaucoma. It decreases intraocular pressure. Adverse effects Side effects of aceclidine include increased salivation and bradycardia (in excessive doses). Mechanism of action Aceclidine acts as a muscarinic acetylcholine receptor agonist. See also * Talsaclidine (drug with a similar structure) * Muscarine Muscarine, L-(+)-muscarine, or muscarin is a natural product found in certain mushrooms, particularly in ''Inocybe'' and ''Clitocybe'' species, such as the deadly '' C. dealbata''. Mushrooms in the genera ''Entoloma'' and ''Mycena'' have al ... References {{Muscarinic acetylcholine receptor modulators Acetate esters Muscarinic agonists Ophthalmology drugs 3-Quinuclidinyl esters Drugs in the Soviet Union Soviet inventions ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1-bromobutane
1-Bromobutane is the organobromine compound with the formula CH3(CH2)3Br. It is a colorless liquid, although impure samples appear yellowish. It is insoluble in water, but soluble in organic solvents. It is a primarily used as a source of the butyl group in organic synthesis. It is one of several isomers of butyl bromide. Synthesis Most 1-bromoalkanes are prepared by free-radical addition of hydrogen bromide to the 1-alkene. These conditions lead to the anti-Markovnikov addition, i.e. give the 1-bromo derivatives. 1-Bromobutane can also be prepared from butanol by treatment with hydrobromic acid: :CH3(CH2)3OH + HBr → CH3(CH2)3Br + H2O Reactions As a primary haloalkane, it is prone to SN2 type reactions. It is commonly used as an alkylating agent. When combined with magnesium metal in dry ether, it gives the corresponding Grignard reagent A Grignard reagent or Grignard compound is a chemical compound with the general formula , where X is a halogen and R is an orga ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sodium Hydrogen Sulfide
Sodium hydrosulfide is the chemical compound with the formula NaHS. This compound is the product of the half-neutralization of hydrogen sulfide () with sodium hydroxide (NaOH). NaSH and sodium sulfide are used industrially, often for similar purposes. Solid NaSH is colorless. The solid has an odor of owing to hydrolysis by atmospheric moisture. In contrast with sodium sulfide (), which is insoluble in organic solvents, NaSH, being a 1:1 electrolyte, is more soluble. Structure and properties Crystalline NaHS undergoes two phase transitions. At temperatures above 360 K, NaSH adopts the NaCl structure, which implies that the behaves as a spherical anion owing to its rapid rotation, leading to equal occupancy of eight equivalent positions. Below 360 K, a rhombohedral structure forms, and the sweeps out a discoidal shape. Below 114 K, the structure becomes monoclinic. The analogous rubidium and potassium compounds behave similarly. NaSH has a relatively low melting poi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catalytic 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 reduce or 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 and triple bonds in hydrocarbons. Process Hydrogenation has three components, the unsaturated substrate, the hydrogen (or hydrogen source) and, invariably, a catalyst. The 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 catalysts and conditions that are used for hydrogenation reactions can also lead to isomerization of the alkenes from cis to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Disulfur Dichloride
Disulfur dichloride is the inorganic compound of sulfur and chlorine with the Chemical formula, formula S2Cl2. Some alternative names for this compound are ''sulfur monochloride'' (the name implied by its empirical formula, SCl), ''disulphur dichloride'' (British English Spelling) and ''sulphur monochloride'' (British English Spelling). S2Cl2 has the structure implied by the formula Cl−S−S−Cl, wherein the angle between the Cla−S−S and S−S−Clb planes is 90°. This structure is referred to as ''gauche'', and is akin to that for Hydrogen peroxide, H2O2. A rare isomer of S2Cl2 is S=SCl2; this isomer forms transiently when S2Cl2 is exposed to UV-radiation (see thiosulfoxides). Synthesis, basic properties, reactions Pure disulfur dichloride is a yellow liquid that "smokes" in moist air due to reaction with water. An idealized (but complicated) equation is: :16 S2Cl2 + 16 H2O → 8 SO2 + 32 HCl + 3 octasulfur, S8 It is produced by partial chlorination of elemental sulfur. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amyl Nitrite
Amyl nitrite is a chemical compound with the formula C5H11ONO. A variety of isomers are known, but they all feature an amyl group attached to the nitrite functional group. The alkyl group is unreactive and the chemical and biological properties are mainly due to the nitrite group. Like other alkyl nitrites, amyl nitrite is bioactive in mammals, being a vasodilator, which is the basis of its use as a prescription medicine. As an inhalant, it also has a psychoactive effect, which has led to its recreational use, with its smell being described as that of old socks or dirty feet. It is also referred to as ''banapple gas''. It was first documented in 1844 and came into medical use in 1867. Uses * Amyl nitrite is employed medically to treat heart diseases as well as angina. * Amyl nitrite is sometimes used as an antidote for cyanide poisoning. It can act as an oxidant, to induce the formation of methemoglobin. Methemoglobin in turn can sequester cyanide as cyanomethemoglobin. * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catalytic 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 reduce or 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 and triple bonds in hydrocarbons. Process Hydrogenation has three components, the unsaturated substrate, the hydrogen (or hydrogen source) and, invariably, a catalyst. The 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 catalysts and conditions that are used for hydrogenation reactions can also lead to isomerization of the alkenes from cis to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
