依他唑酯

依他唑酯(英语:Etazolate,开发代号:SQ-20,009EHT-0202),也叫乙酰腙吡唑啶,是一种抗焦虑药物,是吡唑并吡啶衍生物,具有独特的药理特性。[1][2][3]它作为巴比妥结合位点GABAA受体正向变构调节剂[4][5][6][7]A1A2亚型的腺苷拮抗剂[8]以及对PDE4同工型具有选择性的磷酸二酯酶抑制剂[9][10][11]该药物目前正处于治疗阿尔茨海默病的临床试验中。[12]

依他唑酯
臨床資料
给药途径口服
ATC碼
  • 未分配
法律規範狀態
法律規範
  • 不受管制
识别
  • Ethyl 1-ethyl-4-[2-(propan-2-ylidene)hydrazinyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxylate
CAS号51022-77-6
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
化学
化学式C14H19N5O2
摩尔质量289.34 g·mol−1
3D模型(JSmol
  • CCN1C2=NC=C(C(=C2C=N1)NN=C(C)C)C(=O)OCC
  • InChI=1S/C14H19N5O2/c1-5-19-13-10(8-16-19)12(18-17-9(3)4)11(7-15-13)14(20)21-6-2/h7-8H,5-6H2,1-4H3,(H,15,18)
  • Key:OPQRBXUBWHDHPQ-UHFFFAOYSA-N

参见

参考资料

  1. Hall JA, Morton I. . Kluwer Academic. 1999. ISBN 0-7514-0499-3.
  2. Williams M. . Journal of Medicinal Chemistry. May 1983, 26 (5): 619–628. PMID 6132997. doi:10.1021/jm00359a001.
  3. Williams M, Risley EA. . Life Sciences. February 1979, 24 (9): 833–841. PMID 449623. doi:10.1016/0024-3205(79)90367-9.
  4. Zezula J, Slany A, Sieghart W. . European Journal of Pharmacology. April 1996, 301 (1–3): 207–214. PMID 8773466. doi:10.1016/0014-2999(96)00066-0.
  5. Davies MF. . Remington G, Baskys A (编). . Boca Raton: CRC Press. 1996. ISBN 0-8493-8386-2.
  6. Olsen RW, Gordey M. . Mishina M, Kurachi Y (编). . Handbook of Experimental Pharmacology 147. Berlin: Springer. 2000: 499–517. ISBN 3-540-66127-1. doi:10.1007/978-3-642-57083-4_19.
  7. Olsen RW. . Jucker E (编). 31. Boston: Birkhauser. 1987: 526. ISBN 3-7643-1837-6.
  8. Williams M, Jarvis MF. . Pharmacology, Biochemistry, and Behavior. February 1988, 29 (2): 433–441. PMID 3283781. S2CID 35635747. doi:10.1016/0091-3057(88)90182-7.
  9. Chasin M, Harris DN, Phillips MB, Hess SM. . Biochemical Pharmacology. September 1972, 21 (18): 2443–2450. PMID 4345859. doi:10.1016/0006-2952(72)90414-5.
  10. Wang P, Myers JG, Wu P, Cheewatrakoolpong B, Egan RW, Billah MM. . Biochemical and Biophysical Research Communications. May 1997, 234 (2): 320–324. PMID 9177268. doi:10.1006/bbrc.1997.6636.
  11. Daniel JL. . Gresele P (编). . Cambridge, UK: Cambridge University Press. 2002. ISBN 0-521-80261-X.
  12. . Pipeline. ExonHit. (原始内容存档于2011-01-11).
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