卡他唑酯

卡他唑酯
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 Уthyl 4-(butylamino)-1-ethyl-1H-pyrazolo[3,4-b]pyridine-5-carboxylate; ;
CAS号	34966-41-1
PubChem CID	37015;
ChemSpider	33966;
UNII	8K93Z46WPY;
ChEMBL	ChEMBL8184;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID20188511 ;
化学信息
化学式	C15H22N4O2
摩尔质量	290.37 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(C1=CN=C(N(CC)N=C2)C2=C1NCCCC)OCC;

卡他唑酯（英语：Cartazolate，开发代号：SQ-65,396）是一种吡唑并吡啶类药物。它作为复合物巴比妥结合位点的 GABA_A受体正向变构调节剂，对动物具有抗焦虑作用。^[1]^[2]^[3]^[4]它还可作为A₁和A₂亚型的腺苷拮抗剂以及磷酸二酯酶抑制剂。^[5]^[6]卡他唑酯经过人体临床试验，发现对焦虑症有效，但从未上市。^[7]它是由E.R. Squibb and Sons的团队于1970年代开发的。^[8]

参见

参考资料

^ Placheta P, Karobath M. In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes. European Journal of Pharmacology. March 1980, 62 (2–3): 225–8. PMID 6103810. doi:10.1016/0014-2999(80)90281-2.
^ Supavilai P, Karobath M. Action of pyrazolopyridines as modulators of [3H]flunitrazepam binding to the gaba/benzodiazepine receptor complex of the cerebellum. European Journal of Pharmacology. March 1981, 70 (2): 183–93. PMID 6114867. doi:10.1016/0014-2999(81)90213-2.
^ Leeb-Lundberg F, Snowman A, Olsen RW. Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites. Journal of Neuroscience. May 1981, 1 (5): 471–7. PMC 6564167  . PMID 7050308. doi:10.1523/JNEUROSCI.01-05-00471.1981  .
^ Bristow DR, Martin IL. Biochemical characterization of an isolated and functionally reconstituted gamma-aminobutyric acid/benzodiazepine receptor. Journal of Neurochemistry. March 1990, 54 (3): 751–61. PMID 2154549. S2CID 25784613. doi:10.1111/j.1471-4159.1990.tb02315.x.
^ Daly JW, Hong O, Padgett WL, Shamim MT, Jacobson KA, Ukena D. Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors. Biochemical Pharmacology. February 1988, 37 (4): 655–64. PMC 3445624  . PMID 2829919. doi:10.1016/0006-2952(88)90139-6.
^ Wachtel H. Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors. Psychopharmacology. 1982, 77 (4): 309–16. PMID 6182575. S2CID 10122417. doi:10.1007/BF00432761.
^ O'Brien, Robert. Receptor binding in drug research. New York: Dekker. 1986: 519. ISBN 0-8247-7548-1.
^ US 3966746,Hoehn, Hans & Theodor Denzel,「Amino derivatives of pyrazolopyridine carboxamides」,发表于1976-06-29

[pmid6103810-1] Placheta P, Karobath M. In vitro modulation by SQ 20009 and SQ 65396 of GABA receptor binding in rat CNS membranes. European Journal of Pharmacology. March 1980, 62 (2–3): 225–8. PMID 6103810. doi:10.1016/0014-2999(80)90281-2.

[pmid6114867-2] Supavilai P, Karobath M. Action of pyrazolopyridines as modulators of [3H]flunitrazepam binding to the gaba/benzodiazepine receptor complex of the cerebellum. European Journal of Pharmacology. March 1981, 70 (2): 183–93. PMID 6114867. doi:10.1016/0014-2999(81)90213-2.

[pmid7050308-3] Leeb-Lundberg F, Snowman A, Olsen RW. Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites. Journal of Neuroscience. May 1981, 1 (5): 471–7. PMC 6564167  . PMID 7050308. doi:10.1523/JNEUROSCI.01-05-00471.1981  .

[pmid2154549-4] Bristow DR, Martin IL. Biochemical characterization of an isolated and functionally reconstituted gamma-aminobutyric acid/benzodiazepine receptor. Journal of Neurochemistry. March 1990, 54 (3): 751–61. PMID 2154549. S2CID 25784613. doi:10.1111/j.1471-4159.1990.tb02315.x.

[pmid2829919-5] Daly JW, Hong O, Padgett WL, Shamim MT, Jacobson KA, Ukena D. Non-xanthine heterocycles: activity as antagonists of A1- and A2-adenosine receptors. Biochemical Pharmacology. February 1988, 37 (4): 655–64. PMC 3445624  . PMID 2829919. doi:10.1016/0006-2952(88)90139-6.

[pmid6182575-6] Wachtel H. Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', 5'-monophosphate phosphodiesterase inhibitors. Psychopharmacology. 1982, 77 (4): 309–16. PMID 6182575. S2CID 10122417. doi:10.1007/BF00432761.

[isbn0-8247-7548-1-7] O'Brien, Robert. Receptor binding in drug research. New York: Dekker. 1986: 519. ISBN 0-8247-7548-1.

[8] US 3966746,Hoehn, Hans & Theodor Denzel,「Amino derivatives of pyrazolopyridine carboxamides」,发表于1976-06-29

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]