Pharmacokinetics and distribution of cathine and cathinone in rats.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology(2022)

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摘要
Khat is a stimulant plant that contains stimulant chemicals such as cathine and cathinone, which abuses to induce euphoria, alertness, and motor activity. This study was carried out to determine the pharmacokinetic and distributions of cathine and cathinone following a single dosage of khat extract in rats. Practically, a total of 24 adult male Wistar albino rats aged between 8 and 12 weeks (250-300 g weight) were randomly selected and divided into six groups 4 rats each. After a single dosage (2000 mg/kg body weight) administered by oral gavage, each group was sacrifice at specific time that schedules to be 0.5, 1, 2.5, 5, 12, and 24 hours for group number 1, 2, 3, 4, 5, and 6, respectively. Specimens were obtained as tissues and separated serum for consequences analysis. The mass spectra profiles of the interested analytes were detected by using two different types of liquid chromatography mass spectrometry; (i) Ultra-performance liquid chromatography in coupled with with quadrupole time-of-flight mass spectrometry (UPLC-QTOF/MS) system, (ii) High performance liquid chromatography ion trap mass spectrometry (HPLC-IT/MS) system. Cathine and cathinone were qualified and quantified in serum, brain, lung, heart, liver and kidney following a single khat administration dosage. The highest tissue levels were reach within 0.5 hour in the lung, liver, and heart for cathine and within 0.5 hour in the heart for cathinone. Interestingly, more than 60% of the serum content of cathine and cathinone reached the peak in the brain within 2.5 hours with mean residence time (MRT last) 2.31 - 3.31 hours. Moreover, at the level of the neurotransmitters such as epinephrine, dopamine, norepinephrine and serotonin, their presence were detected in a delayed, prolonged and organ specific manner. This findings provided further basis for experimental, clinical, and forensic studies.
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关键词
cathinone,pharmacokinetics,cathine
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