曲卡唑酯

**曲卡唑酯**
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 4-(butylamino)-1-ethyl-6-methyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylate; ;
CAS号	41094-88-6
PubChem CID	5522;
IUPHAR/BPS	5467;
ChemSpider	5321;
UNII	NH0HPL3U1T;
KEGG	D06200;
ChEBI	CHEBI:92596;
ChEMBL	ChEMBL84567;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID3046956 ;
ECHA InfoCard	100.050.178
化学信息
化学式	C16H24N4O2
摩尔质量	304.39 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(OCC)c1c(c2c(nc1C)n(nc2)CC)NCCCC;
	InChI InChI=1S/C16H24N4O2/c1-5-8-9-17-14-12-10-18-20(6-2)15(12)19-11(4)13(14)16(21)22-7-3/h10H,5-9H2,1-4H3,(H,17,19); Key:PCTRYMLLRKWXGF-UHFFFAOYSA-N;

曲卡唑酯（英语：Tracazolate，开发代号：ICI-136,753）是一种用于科学研究的抗焦虑药物。它是一种吡唑并吡啶衍生物，与扎来普隆等吡唑并嘧啶类药物关系最密切，是结构多样的药物之一，被称为非苯二氮䓬类药物，其作用与苯二氮䓬类药物相同的受体靶点，但具有不同的化学结构。^[1]

曲卡唑酯主要具有抗焦虑和抗惊厥作用，镇静和肌肉松弛作用仅在较高剂量时出现。^[2]它具有独特的受体结合特征，涉及几种GABA_A受体亚型的变构调节，对含有α1和β3亚基的GABA_A受体具有选择性，但根据构成受体复合物的第三种亚基类型表现出不同的效果。^[3]

参见[编辑]

参考资料[编辑]

^ Patel JB, Malick JB, Salama AI, Goldberg ME. Pharmacology of pyrazolopyridines. Pharmacology, Biochemistry, and Behavior. October 1985, 23 (4): 675–80. PMID 2866547. S2CID 31584179. doi:10.1016/0091-3057(85)90436-8.
^ Patel JB, Malick JB. Pharmacological properties of tracazolate: a new non-benzodiazepine anxiolytic agent. European Journal of Pharmacology. March 1982, 78 (3): 323–33. PMID 6121711. doi:10.1016/0014-2999(82)90034-6.
^ Thompson SA, Wingrove PB, Connelly L, Whiting PJ, Wafford KA. Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. Molecular Pharmacology. April 2002, 61 (4): 861–9. PMID 11901225. S2CID 7039885. doi:10.1124/mol.61.4.861.

[1] Patel JB, Malick JB, Salama AI, Goldberg ME. Pharmacology of pyrazolopyridines. Pharmacology, Biochemistry, and Behavior. October 1985, 23 (4): 675–80. PMID 2866547. S2CID 31584179. doi:10.1016/0091-3057(85)90436-8.

[2] Patel JB, Malick JB. Pharmacological properties of tracazolate: a new non-benzodiazepine anxiolytic agent. European Journal of Pharmacology. March 1982, 78 (3): 323–33. PMID 6121711. doi:10.1016/0014-2999(82)90034-6.

[3] Thompson SA, Wingrove PB, Connelly L, Whiting PJ, Wafford KA. Tracazolate reveals a novel type of allosteric interaction with recombinant gamma-aminobutyric acid(A) receptors. Molecular Pharmacology. April 2002, 61 (4): 861–9. PMID 11901225. S2CID 7039885. doi:10.1124/mol.61.4.861.

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