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Ocaperidone
Ocaperidone (R 79598) is a benzisoxazole antipsychotic. It was initially developed by Janssen, later licensed to French laboratory Neuro3D and then acquired in 2007 by German company Evotec. It was found to be more potent than risperidone in animal studies, but its testing was abandoned in 2010 after unfavorable results in human Phase II trials, as while it was effective at controlling symptoms of schizophrenia, ocaperidone produced an unacceptable amount of extrapyramidal side effects.Geerts H, Spiros A, Roberts P, Twyman R, Alphs L, Grace AA. Blinded prospective evaluation of computer-based mechanistic schizophrenia disease model for predicting drug response. ''PLoS One''. 2012;7(12):e49732. Synthesis The last step requires attachment of the sidechain between 3-(2-bromoethyl)-2,9-dimethyl 4H-pyrido ,2-ayrimidin-4-oneCID:18995805(1) and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole 4163-77-9(2) completing the convergent synthesis of Ocaperidone (3).. See also * Benperidol * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ocaperidone Synthesis
Ocaperidone (R 79598) is a benzisoxazole antipsychotic. It was initially developed by Janssen, later licensed to French laboratory Neuro3D and then acquired in 2007 by German company Evotec. It was found to be more potent than risperidone in animal studies, but its testing was abandoned in 2010 after unfavorable results in human Phase II trials, as while it was effective at controlling symptoms of schizophrenia, ocaperidone produced an unacceptable amount of extrapyramidal side effects.Geerts H, Spiros A, Roberts P, Twyman R, Alphs L, Grace AA. Blinded prospective evaluation of computer-based mechanistic schizophrenia disease model for predicting drug response. ''PLoS One''. 2012;7(12):e49732. Synthesis The last step requires attachment of the sidechain between 3-(2-bromoethyl)-2,9-dimethyl 4H-pyrido ,2-ayrimidin-4-oneCID:18995805(1) and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole 4163-77-9(2) completing the convergent synthesis of Ocaperidone (3).. See also * Benperidol * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trifluperidol
Trifluperidol is a typical antipsychotic of the butyrophenone chemical class. It has general properties similar to those of haloperidol, but is considerably more potent by weight, and causes relatively more severe side effects, especially tardive dyskinesia and other extrapyramidal effects. It is used in the treatment of psychoses including mania and schizophrenia. It was discovered at Janssen Pharmaceutica in 1959. Synthesis The Grignard reaction between 1-benzyl-4-piperidone 612-20-2(1) and 3-bromobenzotrifluoride 01-78-5(2) gives 1-benzyl-4-(3-(trifluoromethyl)phenyl)piperidin-4-olCID:12718203(3). 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 ... removes the benzyl protecting group to give 4- -(trifluoromethyl)phenyl4-piperidinol 249-28-7(4). Alkyl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pirenperone
Pirenperone (, , ; developmental code names R-47456, R-50656) is a serotonin receptor antagonist described as an antipsychotic and tranquilizer which was never marketed. It is a relatively selective antagonist of the serotonin 5-HT2 receptors and has been used in scientific research to study the serotonin system. In the 1980s, the drug was found to block the effects of the lysergic acid diethylamide (LSD) in animals, and along with ketanserin, led to the elucidation of the 5-HT2A receptor as the biological mediator of the effects of serotonergic psychedelics. Synthesis The sidechain is formed from the cyclization of 2-aminopyridine with 2-Acetylbutyrolactone (2) in PPA gave 3-(2-hydroxyethyl)-2-methylpyrido ,2-ayrimidin-4-one 1078-67-5(3). Halogenation replaces the hydroxy with the chloride leaving group. Many syntheses do both steps in one-pot with phosphorus oxychloride. The 4-(4-Fluorobenzoyl)Piperidine 6346-57-7has 12 known named uses. The alkylation between 3-( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzisoxazole
1,2-Benzisoxazole is an aromatic organic compound with a molecular formula C7H5NO containing a benzene-fused isoxazole ring structure. The compound itself has no common applications; however, functionalized benzisoxazoles and benzisoxazoyls have a variety of uses, including pharmaceutical drugs such as some antipsychotics (including risperidone, paliperidone, ocaperidone, and iloperidone) and the anticonvulsant zonisamide. Its aromaticity makes it relatively stable; however, it is only weakly basic. Synthesis Benzisoxazole may be prepared from inexpensive salicylaldehyde, via a base catalyzed room temperature reaction with hydroxylamine-''O''-sulfonic acid. : Reactions Kemp elimination First reported by Daniel S. Kemp, the relatively weak N-O bond can be cleaved by a strong base to yield a 2-hydroxybenzonitrile species. See also ;Structural isomers *Benzoxazole *Anthranil Anthranil (2,1-benzisoxazole) is an organic compound with a molecular formula C7H5NO, which feature ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha Blockers
Alpha (uppercase , lowercase ; grc, ἄλφα, ''álpha'', or ell, άλφα, álfa) is the first letter of the Greek alphabet. In the system of Greek numerals, it has a value of one. Alpha is derived from the Phoenician letter aleph , which is the West Semitic word for " ox". Letters that arose from alpha include the Latin letter A and the Cyrillic letter А. Uses Greek In Ancient Greek, alpha was pronounced and could be either phonemically long ( ː or short ( . Where there is ambiguity, long and short alpha are sometimes written with a macron and breve today: Ᾱᾱ, Ᾰᾰ. * ὥρα = ὥρᾱ ''hōrā'' "a time" * γλῶσσα = γλῶσσᾰ ''glôssa'' "tongue" In Modern Greek, vowel length has been lost, and all instances of alpha simply represent the open front unrounded vowel . In the polytonic orthography of Greek, alpha, like other vowel letters, can occur with several diacritic marks: any of three accent symbols (), and either of two breathing marks ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotics
Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as Extrapyramidal symptoms, involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihistamines
Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use. Although people typically use the word "antihistamine" to describe drugs for treating allergies, doctors and scientists use the term to describe a class of drug that opposes the activity of histamine receptors in the body. In this sense of the word, antihistamines are subclassified according to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aban ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2 Antagonists
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets and is rel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benperidol
Benperidol, sold under the trade name Anquil among others, is a typical antipsychotic primarily used to treat hypersexuality syndromes and can be used to treat schizophrenia. It is a highly potent butyrophenone derivative and is the most potent neuroleptic on the European market, with chlorpromazine equivalency as high as 75 to 100 (about 150 to 200% the potency, per dose, of haloperidol). It is sometimes prescribed to sex offenders as a condition of their parole, as an alternative to anti-androgen drugs such as cyproterone acetate. Benperidol was discovered by Janssen Pharmaceutica in 1961 and has been marketed since 1966. It is mainly used in Germany, but it is also available in Belgium, Greece, Italy, the Netherlands, and the United Kingdom. Pharmacology Pharmacodynamics Benperidol is a strong dopamine receptor antagonist ( D2 (''K''i 0.027 nM) and D4 (''K''i 0.066 nM)) with weaker serotonin receptor antagonism ( 5-HT2A (''K''i 3.75 nM)). In high doses, it has antihis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotic
Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as Extrapyramidal symptoms, involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convergent Synthesis
In chemistry a convergent synthesis is a strategy that aims to improve the efficiency of multistep synthesis, most often in organic synthesis. In this type of synthesis several individual pieces of a complex molecule are synthesized in stage one, and then in stage two these pieces are combined to form the final product. In linear synthesis the overall yield quickly drops with each reaction step: :A → B → C → D Suppose the yield is 50% for each reaction; the overall yield of D is only 12.5% from A. In a convergent synthesis :A → B (50%) :C → D (50%) :B + D → E (25%) the overall yield of E (25%) looks much better. Convergent synthesis is applied in the synthesis of complex molecules and involves fragment coupling and independent synthesis. This technique is more useful if the compound is large and symmetric, where at least two aspects of the molecule can be formed separately and still come together. Examples: * Convergent synthesis is encountered in dendrimer s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
