티오스피로네

Tiospirone
티오스피로네
Tiospirone.svg
임상 데이터
ATC 코드
  • 없음.
법적 상태
법적 상태
  • 개발 종료
약동학 데이터
대사간염
반감기 제거1.4시간
배설물소변
식별자
  • 84444-(1,2-벤조티아졸-3-일)-아진-1-일]부틸]-8-아자스피로[4.5]데칸-7,9-디온
CAS 번호
PubChem CID
IUPHAR/BPS
켐스파이더
유니
첸블
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C24H32N4O2S
몰 질량440.61g/표준−1

티오스피론([1]BMY-13,859)은 아자피론 계열의 비정형 항정신병 약물이다.1980년대 후반 정신분열증 치료제로 조사되었으며 임상시험에서 전형적인 항정신병 약물과 동등한 효과를 가지지만 추체외 부작용을 [2][3][4][5]일으키지는 않는 것으로 밝혀졌다.그러나 개발은 중단되었고 시판되지 않았다.항정신병 특성을 가진 또 다른 아자피론 유도체인 페로스피론은 티오스피론 [6]후 몇 년 후에 합성 및 측정되었다.그것은 비교해서 더 강력하고 더 선별적인 것으로 발견되었고 대신 [6]상용화 되었다.

약리학

약역학

티오스피론은 5-HT1A 수용체 부분작용제, 5-HT2A, 5-HT2C7 수용체 역작용제 및 D2, D4 및 α-아드레날린1 수용체 [7][8][9][10][11][12]길항제 역할을 한다.

바인딩 프로파일[13]

리셉터 Ki(nM)
5-HT2A 0.06
5-HT2C 9.73
5-HT6 950
5-HT7 0.64
M1 630
M2 180
M3 1290
M4 480
M5 3900
D2. 0.5
D4. 13.6

「 」를 참조해 주세요.

레퍼런스

  1. ^ Yevich JP, New JS, Smith DW, et al. (March 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. doi:10.1021/jm00153a010. PMID 2869146.
  2. ^ Jain AK, Kelwala S, Moore N, Gershon S (April 1987). "A controlled clinical trial of tiaspirone in schizophrenia". International Clinical Psychopharmacology. 2 (2): 129–33. doi:10.1097/00004850-198704000-00006. PMID 2885367.
  3. ^ Moore NC, Meyendorff E, Yeragani V, LeWitt PA, Gershon S (April 1987). "Tiaspirone in schizophrenia". Journal of Clinical Psychopharmacology. 7 (2): 98–101. doi:10.1097/00004714-198704000-00010. 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. p. 313. ISBN 0-88048-681-3.
  6. ^ a b Ishizumi K, Kojima A, Antoku F, Saji I, Yoshigi M (December 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. doi:10.1248/cpb.43.2139. PMID 8582016.
  7. ^ Sumiyoshi T, Suzuki K, Sakamoto H, et al. (February 1995). "Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy". Neuropsychopharmacology. 12 (1): 57–64. doi:10.1016/0893-133X(94)00064-7. PMID 7766287.
  8. ^ Roth BL, Tandra S, Burgess LH, Sibley DR, Meltzer HY (August 1995). "D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs". Psychopharmacology. 120 (3): 365–8. doi:10.1007/BF02311185. PMID 8524985. S2CID 13549491.
  9. ^ Weiner DM, Burstein ES, Nash N, et al. (October 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 (October 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 (October 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. doi:10.1007/s00210-007-0182-6. PMID 17786406. S2CID 29337002.
  12. ^ Newman-Tancredi A, Assié MB, Leduc N, Ormière AM, Danty N, Cosi C (September 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. 8 (3): 341–56. doi:10.1017/S1461145704005000. PMID 15707540.
  13. ^ Roth, BL; Driscol, J (12 January 2011). "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Archived from the original on 8 November 2013. Retrieved 3 December 2013.