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Spirodecanone
Spirodecanone refers to a class of spirocyclic ketones, often studied for their potential applications in medicinal chemistry. One notable example is 1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-one, which has been investigated as a metabolite of neuroleptic agents like Fluspirilene. It has a molecular formula of C₁₃H₁₇N₃O and a melting point of 188-191°C. Synthesis The original synthesis was first disclosed by Paul Janssen, and was covered by Daniel Lednicer in one of his books. A recent synthesis of spirodecanone is disclosed: The Strecker-like condensation between N-benzyl-4-piperidone [3612-20-2] (1), aniline and TMSCN [7677-24-9], gives 4-anilino-1-benzylpiperidine-4-carbonitrile [968-86-5] (2). Acid catalyzed partial hydrolysis of the nitrile to the amide afforded 4-anilino-1-benzylpiperidine-4-carboxamide [1096-03-3] (3). Reaction with forms the spiroimidazolidone ring giving 8-benzyl-1-phenyl-1,3,8-triazaspiro[4.5]dec-2-en-4-one [974-42-5] (4). The imine bond is red ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiramide
Spiramide (developmental code name AMI-193) is an experimental antipsychotic that acts as a selective 5-HT2A, 5-HT1A, and D2 receptor antagonist. It has negligible affinity for the 5-HT2C receptor. See also *Spirodecanone Spirodecanone refers to a class of spirocyclic ketones, often studied for their potential applications in medicinal chemistry. One notable example is 1-Phenyl-1,3,8-triazaspiro .5ecan-4-one, which has been investigated as a metabolite of neurol ... References Butyrophenone antipsychotics 4-Fluorophenyl compounds Lactams Nitrogen heterocycles Phenol ethers Spiro compounds Heterocyclic compounds with 2 rings {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiperone
Spiperone, also known as spiroperidol and sold under the brand name Spiropitan (( JP)) is a typical antipsychotic of the butyrophenone family related to haloperidol. It is approved for clinical use in Japan as a treatment for schizophrenia. Pharmacology Spiperone interacts with various monoamine receptors. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl− channels (CaCCs), thus a potential target for therapy of cystic fibrosis. Derivatives ''N''-Methylspiperone (NMSP) is a derivative of spiperone that is used to study the dopamine and serotonin neurotransmitter system. Labeled with the radioisotope carbon-11, it can be used for positron emission tomography. See also * Spirodecanone References {{Navboxes , title = Pharmacodynamics Pharmacodynamics (PD) is the study of the biochemistry, biochemical and physiology, physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluspirilene
Fluspirilene (Redeptin, Imap, R6218) is a diphenylbutylpiperidine typical antipsychotic drug, used for the treatment of schizophrenia. It is administered intramuscularly. It was discovered at Janssen Pharmaceutica in 1963. A 2007 systematic review investigated the efficacy of fluspirilene decanoate for people with schizophrenia: See also * Pimozide * Penfluridol *Spirodecanone * Spiperone * Mosapramine Mosapramine (Cremin) is an atypical antipsychotic used in Japan for the treatment of schizophrenia. It is a potent dopamine antagonist with high affinity to the D2, D3, and D4 receptors, and with moderate affinity for the 5-HT2 receptors. S ... (atypical antipsychotic) References Belgian inventions 1-(4,4-Bis(4-fluorophenyl)butyl)piperidines Janssen Pharmaceutica Typical antipsychotics Spiro compounds Anilines 4-Fluorophenyl compounds {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Paul Janssen
Paul Adriaan Jan, Baron Janssen (12 September 1926 – 11 November 2003) was a Belgian physician. He was the founder of Janssen Pharmaceutica, a pharmaceutical company with over 20,000 employeesPaul Lewi, Obituary of Dr Paul Janssen (1926–2003), Drug Discovery Today, Volume 9, Issue 10, 15 May 2004, Pages 432–433 which became a subsidiary of Johnson & Johnson. Early life and education Janssen was born on 12 September 1926, in Turnhout, to Constant Janssen and Margriet Fleerackers. He attended secondary school at the Jesuit St Jozef college in Turnhout, Belgium after which he decided to follow in his father's footsteps and become a physician. During World War II Janssen studied physics, biology and chemistry at the Facultés universitaires Notre-Dame de la Paix (FUNDP) in Namur. He then studied medicine at the Catholic University of Leuven and Ghent University. In 1951, Janssen received his medical degree ''magna cum laude'' from Ghent University. He graduated with a po ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiro Compounds
In organic chemistry, spiro compounds are compounds that have at least two molecular rings sharing one common atom. Simple spiro compounds are bicyclic (having just two rings). The presence of only one common atom connecting the two rings distinguishes spiro compounds from other bicyclics.For all four categories, see The specific chapters can be found aan respectively, same access date. For the description featuring adjacent atoms for all but the isolated category, see Clayden, op. cit. Spiro compounds may be fully carbocyclic (all carbon) or heterocyclic (having one or more non-carbon atom). One common type of spiro compound encountered in educational settings is a heterocyclic one— the acetal formed by reaction of a diol with a cyclic ketone. The common atom that connects the two (or sometimes three) rings is called the ''spiro atom''. In carbocyclic spiro compounds like spiro .5ndecane, the spiro-atom is a quaternary carbon, and as the ''-ane'' ending implies, these ar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Belgian Inventions
Belgian may refer to: * Something of, or related to, Belgium * Belgians, people from Belgium or of Belgian descent * Languages of Belgium, languages spoken in Belgium, such as Dutch, French, and German *Ancient Belgian language, an extinct language formerly spoken in Gallia Belgica *Belgian Dutch or Flemish, a variant of Dutch *Belgian French, a variant of French *Belgian horse (other), various breeds of horse *Belgian waffle, in culinary contexts * SS ''Belgian'', a cargo ship in service with F Leyland & Co Ltd from 1919 to 1934 *''The Belgian'', a 1917 American silent film See also * *Belgica (other) Gallia Belgica was a province of the Roman Empire covering present-day Luxembourg and parts of France, Belgium and the Netherlands. Belgica may also refer to: Places * Belgica Glacier, Antarctica * Belgica Guyot, an undersea tablemount off An ... * Belgic (other) {{Disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro65-6570
Ro65-6570 is an opioid drug. It has a potential use in preventing the addiction to other opioids. Mechanism of action Ro65-6570 is an opioid drug, it works by activating opioid receptors. However, instead of acting at the mu, kappa and delta receptors, it is instead an agonist at the nociceptin receptor. Potential uses Analgesic Ro65-6570 has analgesic properties. In rats, it is able to reduce cancer pain. It is also able to reduce pain caused by arthritis. Prevention of opioid addiction While being an opioid agonist, Ro65-6570 did not display addictive properties, it instead reduced the addictive properties of other opioids, but did not affect the analgesic effect of those. This could make it useful if combined with more potent opioids, for example oxycodone and Ro65-6570 would reduce pain, but would be less addictive, unlike oxycodone alone. This effect was antagonized by the nociceptin receptor antagonist An antagonist is a character in a story who is prese ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ro64-6198
Ro64-6198 is an opioid drug used in scientific research. It acts as a potent and selective agonist for the nociceptin receptor, also known as the ORL-1 (opiate receptor like-1) receptor, with over 100x selectivity over the other opioid receptors. It produces anxiolytic effects in animal studies equivalent to those of benzodiazepine drugs, but has no anticonvulsant effects and does not produce any overt effects on behaviour. However it does impair short-term memory, and counteracts stress-induced anorexia. It also has antitussive effects, and reduces the rewarding and analgesic effects of morphine, although it did not prevent the development of dependence. It has been shown to reduce alcohol self-administration in animals and suppressed relapses in animal models of alcoholism, and ORL-1 agonists may have application in the treatment of alcoholism. Ro64-6198 was able to be recognised as a discriminative stimulus by rats distinct from other opioid receptor ligands, but was not able t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spiroxatrine
Spiroxatrine (Spiroxamide, R5188) is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist effects and a relatively weak opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ... action.Leysen J, Tollenaere JP, Koch MHJ, Laduron P. Differentiation of opiate and neuroleptic receptor binding in rat brain. ''European Journal of Pharmacology'' 1977; 43(3):253-267. References 5-HT1A antagonists Abandoned drugs Alpha-2 blockers Benzodioxans Dopamine antagonists Imidazolidinones Spiro compounds {{Nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
R6890
R6890, sometimes known as spirochlorphine, is an opioid analgesic and a member of the spiropiperidine family of agents. The first known mention of this compound was in 1977. It has been advertised online as a research chemical having a potency 2-5 times that of fentanyl. Other examples of agents from this class are Ro64-6198 and Ro65-6570. Brorphine also has a similar structure. A precursor chemical used in the synthesis of R6890 is 1-phenyl-1,3,8-triazaspiro(4,5)decan-4-one (also known as spirodecanone), which is used in the synthesis of other drugs including spirilene, fluspirilene, spiramide, spiperone, RP-23618, spioxatrine, L008716 and R5260. Pharmacology The pharmacology of R6890 is described as a nociceptin receptor (NOP) agonist, although R6890 retains significant affinity at the mu opioid receptor. R6890 has affinities (Ki values) of 4, 75, and 10 nM for the mu, delta, and the total opioid receptor population, respectively. See also *Cychlorphine *List of orp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
