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依他唑酯

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
识别信息
  • 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（英语：CompTox Chemicals Dashboard） (EPA)
化学信息
化学式C14H19N5O2
摩尔质量289.34 g·mol−1
3D模型（JSmol（英语：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

依他唑酯（英语：Etazolate，开发代号：SQ-20,009、EHT-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受体的正向变构调节剂、[4][5][6][7]A1和A2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]

参见

参考资料

  1. ^ Hall JA, Morton I. Concise dictionary of pharmacological agents: properties and synonyms. Kluwer Academic. 1999. ISBN 0-7514-0499-3. 
  2. ^ Williams M. Anxioselective anxiolytics. Journal of Medicinal Chemistry. May 1983, 26 (5): 619–628. PMID 6132997. doi:10.1021/jm00359a001. 
  3. ^ Williams M, Risley EA. Enhancement of the binding of 3H-diazepam to rat brain membranes in vitro by SQ 20009, A novel anxiolytic, gamma-aminobutyric acid (GABA) and muscimol. 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. Interaction of allosteric ligands with GABAA receptors containing one, two, or three different subunits. European Journal of Pharmacology. April 1996, 301 (1–3): 207–214. PMID 8773466. doi:10.1016/0014-2999(96)00066-0. 
  5. ^ Davies MF. The Pharmacology of the Gamma-Aminobutyric Acid System. Remington G, Baskys A (编). Brain mechanisms and psychotropic drugs. Boca Raton: CRC Press. 1996. ISBN 0-8493-8386-2. 
  6. ^ Olsen RW, Gordey M. GABAA Receptor Chloride Ion Channels. Mishina M, Kurachi Y (编). Pharmacology of ionic channel function: activators and inhibitors. 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. GABA-Drug Interactions. Jucker E (编). Progress in Drug Research 31. Boston: Birkhauser. 1987: 526. ISBN 3-7643-1837-6. 
  8. ^ Williams M, Jarvis MF. Adenosine antagonists as potential therapeutic agents. 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. 1-Ethyl-4-(isopropylidenehydrazino)-1H-pyrazolo-(3,4-b)-pyridine-5-carboxylic acid, ethyl ester, hydrochloride (SQ 20009)--a potent new inhibitor of cyclic 3',5'-nucleotide phosphodiesterases. 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. Expression, purification, and characterization of human cAMP-specific phosphodiesterase (PDE4) subtypes A, B, C, and D. Biochemical and Biophysical Research Communications. May 1997, 234 (2): 320–324. PMID 9177268. doi:10.1006/bbrc.1997.6636. 
  11. ^ Daniel JL. Platelet signalling; cAMP and cGMP. Gresele P (编). Platelets in thrombotic and non-thrombotic disorders: pathophysiology, pharmacology and therapeutics. Cambridge, UK: Cambridge University Press. 2002. ISBN 0-521-80261-X. 
  12. ^ EHT 0202. Pipeline. ExonHit. （原始内容存档于2011-01-11）. 
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