Tiospiron
IUPAC ime | |
---|---|
8-[4-[4-(1,2-benzotiazol-3-il)piperazin-1-il]butil]-8-azaspiro[4.5]dekan-7,9-dion | |
Farmakokinetički podaci | |
Metabolizam | Hepatic |
Poluvreme eliminacije | 1,4 sata |
Izlučivanje | Urine |
Identifikatori | |
CAS broj | 87691-91-6 Y |
ATC kod | none |
PubChem | CID 55752 |
IUPHAR/BPS | 101 |
ChemSpider | 50348 |
UNII | 35C6UMO5SR Y |
ChEMBL | CHEMBL35057 |
Hemijski podaci | |
Formula | C24H32N4O2S |
Molarna masa | 440,60 g/mol |
Tiospiron (BMY-13,859, tiaspiron, tiosperon) je atipični antipsihotik iz azapironske klase.[1] On je istraživan kao tretman za šizofreniju tokom kasnih 1980-tih i poznato je da je efektivan ekvivalent tipičnih antipsihotika i da ne izaziva ekstrapiramidalne nuspojave.[2][3][4][5] Međutim, njegov razvoj je zaustavljen. Perospiron, jedan drugi derivat azapirona sa antipsihotičkim svojstvima, je sintetisan i karakterisan nekoliko godina kasnije.[6] Za njega je utvrđeno da je potentniji i selektivniji od tiospirona te je plasiran na tržište.[6]
Tiospiron deluje kao parcijalni agonist 5-HT1A receptora, inverzni agonist 5-HT2A, 5-HT2C, i 5-HT7 receptora, i antagonist D2, D4, i α1-adrenergičkog receptora.[7][8][9][10][11][12]
Vidi još
Reference
- ^ Yevich JP; New JS; Smith DW; et al. (1986). „Synthesis and biological evaluation of 1-(1,2-benzisothiazol-3-yl)- and (1,2-benzisoxazol-3-yl)piperazine derivatives as potential antipsychotic agents”. Journal of Medicinal Chemistry. 29 (3): 359—69. PMID 2869146. doi:10.1021/jm00153a010.
- ^ Jain AK, Kelwala S, Moore N, Gershon S (1987). „A controlled clinical trial of tiaspirone in schizophrenia”. International Clinical Psychopharmacology. 2 (2): 129—33. PMID 2885367. doi:10.1097/00004850-198704000-00006.
- ^ Moore NC, Meyendorff E, Yeragani V, LeWitt PA, Gershon S (1987). „Tiaspirone in schizophrenia”. Journal of Clinical Psychopharmacology. 7 (2): 98—101. PMID 3294920.
- ^ Borison RL, Sinha D, Haverstock S, McLarnon MC, Diamond BI (1989). „Efficacy and safety of tiospirone vs. haloperidol and thioridazine in a double-blind, placebo-controlled trial”. Psychopharmacology Bulletin. 25 (2): 190—3. PMID 2574893.
- ^ Nasrallah, Henry A.; Shriqui, Christian L (1995). Contemporary issues in the treatment of schizophrenia. Washington, DC: American Psychiatric Press. str. 313 [/863]. ISBN 0-88048-681-3.
- ^ а б Ishizumi K, Kojima A, Antoku F, Saji I, Yoshigi M (1995). „Succinimide derivatives. II. Synthesis and antipsychotic activity of N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1,2-cis- cyclohexanedicarboximide (SM-9018) and related compounds”. Chemical & Pharmaceutical Bulletin. 43 (12): 2139—51. PMID 8582016. doi:10.1248/cpb.43.2139.
- ^ Sumiyoshi T; Suzuki K; Sakamoto H; et al. (1995). „Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy”. Neuropsychopharmacology. 12 (1): 57—64. PMID 7766287. doi:10.1016/0893-133X(94)00064-7.
- ^ Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY (1995). „D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs”. Psychopharmacology. 120 (3): 365—8. PMID 8524985. doi:10.1007/BF02311185.
- ^ Weiner DM; Burstein ES; Nash N; et al. (2001). „5-hydroxytryptamine2A receptor inverse agonists as antipsychotics”. The Journal of Pharmacology and Experimental Therapeutics. 299 (1): 268—76. PMID 11561089.
- ^ Herrick-Davis K, Grinde E, Teitler M (2000). „Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors”. The Journal of Pharmacology and Experimental Therapeutics. 295 (1): 226—32. PMID 10991983.
- ^ Rauly-Lestienne I, Boutet-Robinet E, Ailhaud MC, Newman-Tancredi A, Cussac D (2007). „Differential profile of typical, atypical and third generation antipsychotics at human 5-HT7a receptors coupled to adenylyl cyclase: detection of agonist and inverse agonist properties”. Naunyn-Schmiedeberg's Archives of Pharmacology. 376 (1–2): 93—105. PMID 17786406. doi:10.1007/s00210-007-0182-6. ISBN.
- ^ Newman-Tancredi A, Assié MB, Leduc N, Ormière AM, Danty N, Cosi C (2005). „Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia”. The International Journal of Neuropsychopharmacology / Official Scientific Journal of the Collegium Internationale Neuropsychopharmacologicum (CINP). 8 (3): 341—56. PMID 15707540. doi:10.1017/S1461145704005000.
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Butirofenoni: Azaperon · Benperidol · Bromperidol · Droperidol · Fluanizon · Haloperidol # · Lenperon · Moperon · Pipamperon · Spiperon · Timiperon · Trifluperidol
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Tioksanten: Hlorprotiksen · Klopentiksol · Flupentiksol · Tiotiksen · Zuklopentiksol
Triciklici: Butaklamol · Fluotracen · Loksapin · Trimipramin
Drugi: ProtipendilButirofenoni: Cinuperon · Melperon · Setoperon
Benzo(izo)oksazolpiperidini: Iloperidon · Okaperidon · Paliperidon · Rispolept #
Benzo(izo)tiazolpiperazini: Lurasidon · Perospiron · Revospiron · Tiospiron · Ziprasidon
Difenilbutilpiperazini: Amperozid
Fenilpiperazini: Aripiprazol · Bifeprunoks · Brekspiprazol† · Elopiprazol · Umespiron
Triciklici: Amoksapin · Asenapin · Karpipramin · Klocapramin · Klorotepin · Klotiapin · Klozapin # · Fluperlapin · Gevotrolin · Metitepin · Mosapramin · NDMC · Olanzapin · Pihindon · Kvetijapin · Tenilapin · Zotepin
Drugi: Blonanserin · Kariprazin · Molindon · Pimavanserin · Roksindol · Sarizotan · Sertindol · Spiramid · Zikronapin†Molimo Vas, obratite pažnju na važno upozorenje u vezi sa temama iz oblasti medicine (zdravlja). |