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  • 开思酮

    Cathinone

    开思酮
    产品编号 CFN00058
    CAS编号 71031-15-7
    分子式 = 分子量 C9H11NO = 149.19
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源 The herbs of Catha edulis
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    开思酮 CFN00058 71031-15-7 1mg QQ客服:215959384
    开思酮 CFN00058 71031-15-7 5mg QQ客服:215959384
    开思酮 CFN00058 71031-15-7 10mg QQ客服:215959384
    开思酮 CFN00058 71031-15-7 20mg QQ客服:215959384
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
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    IF=12.804(2019)

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  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Food Bioscience2023, 56:103311.
  • Antioxidants (Basel).2021, 10(10):1620.
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  • TCI CO.2019, US20190151281A1
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  • Molecules.2019, 24(10):E1926
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  • ...
  • 生物活性
    Description: Cathinone is the main psychoactive constituent of the khat leaf and this alkaloid is a natural amphetamine, cathinone shares the action of amphetamine on CNS as well as its sympathomimetic effects, it induces significant behavioral changes and CNS activation in the hamster by systemic administration.Cathinone has amphetamine-like effects, it can produce increases in blood pressure and in heart rate, and these changes are concomitant with the presence of cathinone in blood plasma, it has in humans euphorigenic and psychostimulant effects. Cathinone has vasoconstrictor activity which is not due to indirect or direct sympathomimetic activity, the coronary vasoconstriction may explain the increased incidence of myocardial infarction in khat chewers, which may arise from coronary vasospasm.
    Targets: NMDAR
    In vitro:
    Auton Autacoid Pharmacol. 2003 Oct-Dec;23(5-6):319-26.
    Coronary and aortic vasoconstriction by cathinone, the active constituent of khat.[Pubmed: 15255816 ]
    1. The psychostimulant constituent of khat leaves, S-(-)-cathinone, was examined for vascular activity on the coronary vasculature of guinea-pig-isolated perfused hearts and aortic ring preparations.
    METHODS AND RESULTS:
    2. Cathinone caused coronary vasoconstriction, negative inotropy and negative chronotropy in isolated hearts. The major metabolite of cathinone after its ingestion, 1R.2S-(-)-norephedrine (norephedrine), also caused coronary vasoconstriction comparable with that by cathinone. Norephedrine, however, had no effect on force or rate of cardiac contractions. 3. Cocaine (10 microm) potentiated the coronary vasoconstriction and positive inotropy by noradrenaline indicating inhibition of neuronal uptake. The vasoconstriction and negative inotropy by cathinone, however, were not affected, indicating that its action was not via release of noradrenaline from sympathetic neurones. 4. The alpha(1)-adrenoceptor antagonist, prazosin, blocked the vasoconstriction by noradrenaline, but not that produced by cathinone in the presence of cocaine. This indicates that the coronary vasoconstriction by cathinone was not due to an action on alpha(1)-adrenoceptors either directly or indirectly through noradrenaline release. 5. Three repeated doses of cathinone displayed the same coronary vasoconstrictor responses, indicating a lack of tachyphylaxis and therefore confirming that the response was unlikely to be due to indirect sympathomimetic activity through release of noradrenaline. 6. In guinea-pig aortic rings, the order of vasoconstrictor activity was: noradrenaline > norephedrine > cathinone, with each causing approximately equivalent maximum responses. The time to reach plateau contractions was shortest for noradrenaline (5.1 +/- 0.5 min), then norephedrine (9.3 +/- 1.5 min) and cathinone the longest (25.4 +/- 3.2 min, 335 microm dose).
    CONCLUSIONS:
    7 These results indicate that cathinone has vasoconstrictor activity which is not due to indirect or direct sympathomimetic activity. The precise mechanism for this vasoconstriction remains to be determined. The coronary vasoconstriction may explain the increased incidence of myocardial infarction in khat chewers, which may arise from coronary vasospasm.
    In vivo:
    Eur J Pharmacol. 2015 Jul 5;758:142-6.
    Direct and indirect cardiovascular actions of cathinone and MDMA in the anaesthetized rat.[Pubmed: 25863258]
    The stimulants cathinone (from Khat leaves) and methylenedioxymeth-amphetamine (MDMA) produce adrenoceptor mediated tachycardia and vasopressor actions that may be the result of direct receptor stimulation, actions on the noradrenaline transporter, and/or displacement of noradrenaline from nerve terminals.
    METHODS AND RESULTS:
    Effects of cathinone or MDMA were compared with those of the indirect sympathomimetic tyramine. Male Wistar rats were anaesthetized with pentobarbitone for blood pressure and heart rate recording. Some rats were sympathectomised by treatment with 6-hydroxydopamine. In the anaesthetised rat, cathinone, MDMA and tyramine (all 0.001-1 mg/kg) produced marked tachycardia, tyramine produced marked pressor responses and MDMA produced small pressor responses. The tachycardia to cathinone and MDMA was almost abolished by propranolol (1mg/kg). Pretreatment with cocaine (1mg/kg) did not significantly affect the tachycardia to cathinone or MDMA, but reduced the response to tyramine. However, in sympathectomised rats, the tachycardia to cathinone or MDMA was markedly attenuated, but the tachycardia to tyramine was only partially reduced. Blood pressure effects of tyramine and MDMA were also markedly attenuated by sympathectomy.
    CONCLUSIONS:
    The results demonstrate firstly that cocaine may not be the most suitable agent for assessing direct versus indirect agonism in cardiovascular studies. Secondly, the use of chemical sympathectomy achieved the desired goal of demonstrating that cardiac β-adrenoceptor mediated actions of cathinone and MDMA are probably largely indirect.
    Neurosci Lett. 2014 Jan 24;559:34-8.
    Cathinone increases body temperature, enhances locomotor activity, and induces striatal c-fos expression in the Siberian hamster.[Pubmed: 24287379]
    Cathinone is a β-keto alkaloid that is the major active constituent of khat, the leaf of the Catha edulis plant that is chewed recreationally in East Africa and the Middle East. Related compounds, such as methCathinone and mephedrone have been increasing in popularity as recreational drugs, resulting in the recent proposal to classify khat as a Class C drug in the UK. There is still limited knowledge of the pharmacological effects of Cathinone.
    METHODS AND RESULTS:
    This study examined the acute effects of Cathinone on core body temperature, locomotor and other behaviors, and neuronal activity in Siberian hamsters. Adult male hamsters, previously implanted with radio telemetry devices, were treated with Cathinone (2 or 5mg/kg i.p.), the behavioral profile scored and core body temperature and locomotor activity recorded by radio telemetry. At the end of the study, hamsters received vehicle or Cathinone (5mg/kg) and neuronal activation in the brain was determined using immunohistochemical evaluation of c-fos expression. Cathinone dose-dependently induced significant (p<0.0001) increases in both temperature and locomotor activity lasting 60-90min. Cathinone (2mg/kg) increased rearing (p<0.02), and 5mg/kg increased both rearing (p<0.001) and lateral head twitches (p<0.02). Both Cathinone doses decreased the time spent at rest (p<0.001). The number of c-fos immunopositive cells were significantly increased in the striatum (p<0.0001) and suprachiasmatic nucleus (p<0.05) following Cathinone, indicating increased neuronal activity. There was no effect of Cathinone on food intake or body weight.
    CONCLUSIONS:
    It is concluded that systemic administration of Cathinone induces significant behavioral changes and CNS activation in the hamster.
    Pharmacol Toxicol. 1992 Feb;70(2):77-86.
    Cathinone, a natural amphetamine.[Pubmed: 1508843]
    Cathinone is an alkaloid that has been discovered some fifteen years ago in the leaves of the khat bush. This plant grows in East Africa and in southern Arabia, and the inhabitants of these regions frequently chew khat because of its stimulating properties.
    METHODS AND RESULTS:
    Cathinone, which is S(-)-alpha-aminopropiophenone, was soon found to have a pharmacological profile closely resembling that of amphetamine; indeed, in a wide variety of in vitro and in vivo experiments it was demonstrated that cathinone shares the action of amphetamine on CNS as well as its sympathomimetic effects; thus, for example, drug-conditioned animals will not distinguish between cathinone and amphetamine. These various observations were confirmed by a clinical experiment showing that cathinone also in humans produces amphetamine-like objective and subjective effects. Finally, it was demonstrated that cathinone operates through the same mechanism as amphetamine, i.e. it acts by releasing catecholamines from presynaptic storage sites.
    CONCLUSIONS:
    Thus, much experimental evidence indicates that cathinone is the main psychoactive constituent of the khat leaf and that, in fact, this alkaloid is a natural amphetamine.
    Br J Clin Pharmacol. 1990 Dec;30(6):825-8.
    Amphetamine-like effects in humans of the khat alkaloid cathinone.[Pubmed: 2288828 ]
    1. The chewing of khat leaves as a stimulant is common in certain countries, and the effects of this material are supposed to be due to the phenylalkylamine alkaloid cathinone.
    METHODS AND RESULTS:
    In order to determine the effects of this substance in humans, a single oral dose of cathinone or placebo was administered to six healthy male volunteers in a double-blind, random order crossover study. 2. Cathinone produced increases in blood pressure and in heart rate, and these changes were concomitant with the presence of cathinone in blood plasma. 3. The physical and mental changes that the subjects reported during the experiment indicated that cathinone has in humans euphorigenic and psychostimulant effects.
    CONCLUSIONS:
    4. These observations support the assumption that cathinone is the constituent mainly responsible for the effects of khat, and they show that this alkaloid has also in humans amphetamine-like effects.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 6.7029 mL 33.5143 mL 67.0286 mL 134.0572 mL 167.5716 mL
    5 mM 1.3406 mL 6.7029 mL 13.4057 mL 26.8114 mL 33.5143 mL
    10 mM 0.6703 mL 3.3514 mL 6.7029 mL 13.4057 mL 16.7572 mL
    50 mM 0.1341 mL 0.6703 mL 1.3406 mL 2.6811 mL 3.3514 mL
    100 mM 0.067 mL 0.3351 mL 0.6703 mL 1.3406 mL 1.6757 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    Merucathinone; Merucathinone CFN00057 107638-80-2 C11H13NO = 175.23 5mg QQ客服:1413575084
    开思酮; Cathinone CFN00058 71031-15-7 C9H11NO = 149.19 5mg QQ客服:1413575084
    3,4-二甲氧基苯丙胺; 3,4-Dimethoxybenzenepropanamine CFN00059 14773-42-3 C11H17NO2 = 195.26 5mg QQ客服:215959384
    3,5-二溴-4-[3-(二甲胺基)丙氧基]肉桂酸; 3,5-Dibromo-4-[3-(dimethylamino)propoxy]cinnamic acid CFN00072 134276-56-5 C14H17Br2NO3 = 407.1 5mg QQ客服:1457312923
    枯美任; Kuramerine CFN00083 21284-19-5 C28H44NO8+ = 522.66 5mg QQ客服:3257982914
    芥子碱; Sinapine CFN00092 18696-26-9 C16H24NO5+ = 310.36 20mg QQ客服:1413575084
    4-(二甲基氨基)肉桂醛; 4-(Dimethylamino)cinnamaldehyde CFN98120 6203-18-5 C11H13NO = 175.23 20mg QQ客服:1413575084
    4-二甲基氨基肉桂酸; 4-(Dimethylamino)cinnamic acid CFN98183 1552-96-1 C11H13NO2 = 191.23 20mg QQ客服:3257982914
    苯丙氨酸甜菜碱; Phenylalanine betaine CFN98950 56755-22-7 C12H17NO2 = 207.3 5mg QQ客服:1457312923
    N-(2-Hydroxy-4-methoxyphenyl)acetamide; N-(2-Hydroxy-4-methoxyphenyl)acetamide CFN98988 58469-06-0 C9H11NO3 = 181.2 5mg QQ客服:215959384

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