Tiospiron

Из Википедије, слободне енциклопедије
Tiospiron
Tiospirone.png
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 ДаY
ATC kod none
PubChem CID 55752
IUPHAR/BPS 101
ChemSpider 50348
UNII 35C6UMO5SR ДаY
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]

Reference[уреди]

  1. 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. 
  2. 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. 
  3. Moore NC, Meyendorff E, Yeragani V, LeWitt PA, Gershon S (1987). „Tiaspirone in schizophrenia”. Journal of Clinical Psychopharmacology. 7 (2): 98—101. PMID 3294920. 
  4. 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. 
  5. Nasrallah, Henry A.; Shriqui, Christian L (1995). Contemporary issues in the treatment of schizophrenia. Washington, DC: American Psychiatric Press. стр. 313. ISBN 0-88048-681-3.  Пронађени су сувишни параметри: |pages= и |page= (помоћ)
  6. 6,0 6,1 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. 
  7. 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. 
  8. 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. 
  9. 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. 
  10. 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. 
  11. 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. 
  12. 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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