3-羟基芬纳西泮
外观
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CAS号 | 70030-11-4 |
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化学式 | C15H10BrClN2O2 |
摩尔质量 | 365.61 g·mol−1 |
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3-羟基芬纳西泮(英语:3-Hydroxyphenazepam),或叫3-羟基苯那西泮,是一种苯二氮䓬类药物,具有催眠、镇静、抗焦虑和抗惊厥作用。[1]它是芬纳西泮的活性代谢物,[1][2]也是苯二氮䓬类药物前药西那西泮的活性代谢物。[3]相对于芬纳西泮,3-羟基芬纳西泮具有微弱的肌肉松弛特性,但在大多数其他方面大致相当。[1]与其他苯二氮卓类药物一样,3-羟基芬纳西泮可作为GABAA受体苯二氮䓬类位点的正向变构调节剂,EC50值为10.3nM。[4][5][6]它曾作为设计师药物在网上销售。[7][8][9][10]
参见
[编辑]参考资料
[编辑]- ^ 1.0 1.1 1.2 Artur Viktorovich Valʹdman. Drug dependence and emotional behavior: neurophysiological and neurochemical approaches. Consultants Bureau. 31 May 1986. ISBN 978-0-306-10984-3.
- ^ Lukasz Komsta; Monika Waksmundzka-Hajnos; Joseph Sherma. Thin Layer Chromatography in Drug Analysis. CRC Press. 20 December 2013: 299–. ISBN 978-1-4665-0715-9.
- ^ Schukin SI, Zinkovsky VG, Zhuk OV. Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice (PDF). Pharmacol Rep. 2011, 63 (5): 1093–100 [2023-02-14]. PMID 22180351. doi:10.1016/s1734-1140(11)70628-4. (原始内容存档 (PDF)于2022-10-12).
- ^ Phenazepam Pre-Review Report (PDF). World Health Organization (WHO). November 2015 [2023-02-14]. (原始内容存档 (PDF)于2022-01-20).
- ^ Kopanitsa, M. V.; Zbarska, S. M.; Boychuk, Ya. A.; Krishtal, O. A. Modulation of GABA-activated currents by phenazepam and its metabolites in isolated rat purkinje neurons. Neurophysiology. 2000, 32 (3): 192. ISSN 0090-2977. S2CID 32313668. doi:10.1007/BF02506568.
- ^ Golovenko, N. Ya; Larionov, V. B. Pharmacodynamical and Neuroreceptor Analysis of the Permeability of the Blood-Brain Barrier for Derivatives of 1,4-Benzodiazepine. Neurophysiology. 2014, 46 (3): 199–205. ISSN 0090-2977. S2CID 33732669. doi:10.1007/s11062-014-9429-2.
- ^ 3-hydroxyphenazepam. New Synthetic Drugs Database. [2016-05-30]. (原始内容存档于2016-09-28).
- ^ Madeleine Pettersson Bergstrand; Anders Helander; Therese Hansson; Olof Beck. Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays. Drug Testing and Analysis. 2016, 9 (4): 640–645. PMID 27366870. doi:10.1002/dta.2003.
- ^ Moosmann, Bjoern; Bisel, Philippe; Franz, Florian; Huppertz, Laura M.; Auwärter, Volker. Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines – an update comprising adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, metizolam, and nitrazolam. Journal of Mass Spectrometry. 2016, 51 (11): 1080–1089. Bibcode:2016JMSp...51.1080M. ISSN 1096-9888. PMID 27535017. doi:10.1002/jms.3840.
- ^ Manchester, Kieran R.; Maskell, Peter D.; Waters, Laura. Experimental versus theoretical log D7.4, pKa and plasma protein binding values for benzodiazepines appearing as new psychoactive substances (PDF). Drug Testing and Analysis. 2018, 10 (8): 1258–1269 [2023-02-14]. ISSN 1942-7611. PMID 29582576. doi:10.1002/dta.2387. (原始内容存档 (PDF)于2021-08-02).
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