依他唑酯
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| 臨床資料 | |
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| 给药途径 | 口服 |
| ATC碼 |
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| 法律規範狀態 | |
| 法律規範 |
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| 识别信息 | |
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| CAS号 | 51022-77-6 |
| PubChem CID | |
| IUPHAR/BPS | |
| ChemSpider | |
| UNII | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| 化学信息 | |
| 化学式 | C14H19N5O2 |
| 摩尔质量 | 289.34 g·mol−1 |
| 3D模型（JSmol） | |
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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
[编辑]参考资料
[编辑]- ^ Hall JA, Morton I. Concise dictionary of pharmacological agents: properties and synonyms. Kluwer Academic. 1999. ISBN 0-7514-0499-3.
- ^ Williams M. Anxioselective anxiolytics. Journal of Medicinal Chemistry. May 1983, 26 (5): 619–628. PMID 6132997. doi:10.1021/jm00359a001.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ Olsen RW. GABA-Drug Interactions. Jucker E (编). Progress in Drug Research 31. Boston: Birkhauser. 1987: 526. ISBN 3-7643-1837-6.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ EHT 0202. Pipeline. ExonHit. （原始内容存档于2011-01-11）.