Tandospirone is most commonly used as a treatment foranxiety anddepressive disorders, such asgeneralised anxiety disorder anddysthymia respectively.[3] For both indications it usually takes a couple of weeks for therapeutic effects to begin to be seen,[3] although at higher doses more rapid anxiolytic responses have been seen.[4] It has also been used successfully as a treatment forbruxism.[5]
Thecatalytic hydrogenation of cis-5-Norbornene-exo-2,3-dicarboxylic anhydride [129-64-6] (1) gives Norbornane-2exo,3exo-dicarboxylic Acid-anhydride [14166-28-0] (2). Reaction with aqueous ammonia leads to Exo-2,3-norbornanedicarboximide [14805-29-9] (3). Alkylation with 1,4-dibromobutane [110-52-1] (4) givesCID:10661911 (5). Alkylation of the remaining halogen with 2-(1-Piperazinyl)Pyrimidine [20980-22-7] (6) completed the synthesis of Tandospirone (7).
Tandospirone is also known as metanopirone and by the developmental code name SM-3997.[20][21][22][5] It is marketed in Japan under the brand name Sediel.[20][21][22][5]
^Nishitsuji K, To H, Murakami Y, Kodama K, Kobayashi D, Yamada T, et al. (2004). "Tandospirone in the treatment of generalised anxiety disorder and mixed anxiety-depression : results of a comparatively high dosage trial".Clinical Drug Investigation.24 (2):121–126.doi:10.2165/00044011-200424020-00007.PMID17516698.S2CID38339009.{{cite journal}}: CS1 maint: overridden setting (link)
^abc"Tandospirone".Martindale: The Complete Drug Reference. The Royal Pharmaceutical Society of Great Britain. 23 September 2011. Retrieved14 November 2013.
^Sumiyoshi T, Matsui M, Nohara S, Yamashita I, Kurachi M, Sumiyoshi C, et al. (October 2001). "Enhancement of cognitive performance in schizophrenia by addition of tandospirone to neuroleptic treatment".The American Journal of Psychiatry.158 (10):1722–1725.doi:10.1176/appi.ajp.158.10.1722.PMID11579010.{{cite journal}}: CS1 maint: overridden setting (link)
^Tanaka H, Tatsuno T, Shimizu H, Hirose A, Kumasaka Y, Nakamura M (December 1995). "Effects of tandospirone on second messenger systems and neurotransmitter release in the rat brain".General Pharmacology.26 (8):1765–1772.doi:10.1016/0306-3623(95)00077-1.PMID8745167.
^Yabuuchi K, Tagashira R, Ohno Y (2004). "Effects of tandospirone, a novel anxiolytic agent, on human 5-HT1A receptors expressed in Chinese hamster ovary cells (CHO cells)".Biogenic Amines.18 (3):319–328.doi:10.1163/1569391041501933.
^Blier P, Curet O, Chaput Y, de Montigny C (July 1991). "Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine--II. Effects of acute administration of 1-PP and long-term administration of tandospirone on noradrenergic neurotransmission".Neuropharmacology.30 (7):691–701.doi:10.1016/0028-3908(91)90176-C.PMID1681447.S2CID44297577.
^Miller LG, Thompson ML, Byrnes JJ, Greenblatt DJ, Shemer A (October 1992). "Kinetics, brain uptake, and receptor binding of tandospirone and its metabolite 1-(2-pyrimidinyl)-piperazine".Journal of Clinical Psychopharmacology.12 (5):341–345.doi:10.1097/00004714-199210000-00009.PMID1362206.S2CID22449352.
^EP 0082402, Ishizumi K, Antoku F, Asami Y, published 1986, assigned to Sumitomo Chemical Company, Limited)
^CN 101880274A, Zhang J, Li L, published 2010, assigned to PKUCare Southwest Synthetic Pharmaceutical Corp., Ltd.
^Nishioka K, Kanamaru H (June 1992). "14C-labeling of a novel anxiolytic agent tandospirone".Journal of Labelled Compounds and Radiopharmaceuticals.31 (6):427–436.doi:10.1002/jlcr.2580310602.ISSN0362-4803.
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