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Metabolism of the synthetic cannabinoid PX-2 in human liver microsomes
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Hai HEI1, Ying ZHANG2, Duo-qi XU3, Yan-yan WANG2, Shi-yang QIN2, Ji-fen WANG1, *, Wen-fang ZHANG2, *
Acta Pharmaceutica Sinica | 2020, 55(6) : 1201 - 1208
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Acta Pharmaceutica Sinica | 2020, 55(6): 1201-1208
Original Articles
Metabolism of the synthetic cannabinoid PX-2 in human liver microsomes
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Hai HEI1, Ying ZHANG2, Duo-qi XU3, Yan-yan WANG2, Shi-yang QIN2, Ji-fen WANG1, *, Wen-fang ZHANG2, *
Affiliations
  • 1. College of Criminal Science and Technology, People's Public Security University of China, Beijing 100038, China
  • 2. The Judicial Identification Center of Beijing Public Security, Key Laboratory of Forensic Toxicology, Ministry of Public Security, Beijing 100192, China
  • 3. China University of Political Science and Law, Beijing 100091, China
Published: 2020-06-12 doi: 10.16438/j.0513-4870.2019-0872
Outline
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This study was performed to determine the metabolic profile of a new illicit drug, PX-2, in human liver microsomes. Q Exactive™ HF Quadrupole-Orbitrap LC-MS (LC-QE-HF-Orbitrap-MS) was employed to determine the metabolic sites and pathways of phase Ⅰ and phase Ⅱ metabolism. PX-2 was added to a microsomal incubation model to simulate human hepatic metabolism. The results showed that a total of 18 phase Ⅰ metabolites and 3 glucuronidated phase Ⅱ metabolites were generated, with the main metabolic pathways of phase Ⅰ metabolism including amide hydrolysis, fluoropentyl oxidative defluorination, benzyl hydroxylation, and carbazole ring hydroxylation. Based on the type and sites of metabolism, phase Ⅰ metabolites M1.1 (amide hydrolysis), M4.1 (carbazole cyclic hydroxylation), and M3.1 (oxidative defluorinative hydroxylation) are proposed to be potential poisoning markers. The results of this study provide a basis for identification of related drugs and establishment of testing methods in biological samples.

N-(1-amino-1-oxo-3-phenylpropan-2-yl)-1-(5-fluoropentyl)-1H-indazole-3-carboxamide  /  synthetic cannabinoids  /  human liver microsomes  /  metabolic pathway
Hai HEI, Ying ZHANG, Duo-qi XU, Yan-yan WANG, Shi-yang QIN, Ji-fen WANG, Wen-fang ZHANG. Metabolism of the synthetic cannabinoid PX-2 in human liver microsomes[J]. Acta Pharmaceutica Sinica, 2020 , 55 (6) : 1201 -1208 . DOI: 10.16438/j.0513-4870.2019-0872
Year 2020 volume 55 Issue 6
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Article Info
doi: 10.16438/j.0513-4870.2019-0872
  • Receive Date:2019-11-04
  • Online Date:2026-01-21
  • Published:2020-06-12
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History
  • Received:2019-11-04
  • Revised:2020-02-08
Funding
Affiliations
    1. College of Criminal Science and Technology, People's Public Security University of China, Beijing 100038, China
    2. The Judicial Identification Center of Beijing Public Security, Key Laboratory of Forensic Toxicology, Ministry of Public Security, Beijing 100192, China
    3. China University of Political Science and Law, Beijing 100091, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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