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
	IUPAC命名法 Ethyl 1-ethyl-4-[2-(propan-2-ylidene)hydrazinyl]-1H-pyrazolo[3,4-b]pyridine-5-carboxylate; ;
CAS号	51022-77-6
PubChem CID	3277;
IUPHAR/BPS	7336;
ChemSpider	3162;
UNII	I89Y79062L;
ChEBI	CHEBI:138502;
ChEMBL	ChEMBL356388;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID4048434 ;
化学信息
化学式	C14H19N5O2
摩尔质量	289.34 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES CCN1C2=NC=C(C(=C2C=N1)NN=C(C)C)C(=O)OCC;
	InChI 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GABA_A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

^ 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）.

[isbn0-7514-0499-3-1] Hall JA, Morton I. Concise dictionary of pharmacological agents: properties and synonyms. Kluwer Academic. 1999. ISBN 0-7514-0499-3.

[pmid6132997-2] Williams M. Anxioselective anxiolytics. Journal of Medicinal Chemistry. May 1983, 26 (5): 619–628. PMID 6132997. doi:10.1021/jm00359a001.

[pmid449623-3] 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.

[pmid8773466-4] 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.

[isbn0-8493-8386-2-5] 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.

[isbn3-540-66127-1-6] 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.

[isbn3-7643-1837-6-7] Olsen RW. GABA-Drug Interactions. Jucker E (编). Progress in Drug Research 31. Boston: Birkhauser. 1987: 526. ISBN 3-7643-1837-6.

[pmid3283781-8] 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.

[pmid4345859-9] 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.

[pmid9177268-10] 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.

[isbn0-521-80261-X-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.

[urlPipeline_|_ExonHit-12] EHT 0202. Pipeline. ExonHit. （原始内容存档于2011-01-11）.

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