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Dominique Pessayre – One of the best experts on this subject based on the ideXlab platform.

  • Inhibition of microsomal triglyceride transfer protein: Another mechanism for drug-induced steatosis in mice
    Hepatology, 2003
    Co-Authors: Philippe Letteron, Angela Sutton, Abdellah Mansouri, Bernard Fromenty, Dominique Pessayre

    Abstract:

    Although many steatogenic drugs inhibit mitochondrial fatty acid β-oxidation, limited information is available on possible effects on hepatic lipoprotein secretion. In the endoplasmic reticulum (ER) lumen, microsomal triglyceride transfer protein (MTP) lipidates apolipoprotein B (Apo B), to form triglyceride (TG)-rich very low density lipoprotein (VLDL) particles, which follow vesicular flow to the plasma membrane to be secreted, whereas incompletely lipidated Apo B particles are partly degraded. We studied hepatic MTP activity, the lipoproteins present in the ER lumen, and hepatic lipoprotein secretion 4 hours after administration of a single dose of Amineptine (1 mmol/kg), amiodarone (1 mmol/kg), doxycycline (0.25 mmol/kg), tetracycline (0.25 mmol/kg), tianeptine (0.5 mmol/kg), or pirprofen (2 mmol/kg) in mice. These various doses have been shown previously to markedly inhibit fatty acid oxidation after a single dose, and to trigger steatosis either after repeated doses (doxycycline) or a single dose (other compounds) in mice. In the present study, Amineptine, amiodarone, pirprofen, tetracycline, and tianeptine, but not doxycycline, inhibited MTP activity in vitro, decreased ex vivo MTP activity in the hepatic homogenate of treated mice, decreased TG in the luminal VLDL fraction of hepatic microsomes of treated mice, and decreased in vivo hepatic lipoprotein secretion (TG and Apo B). In conclusion, several steatogenic drugs inhibit not only mitochondrial β-oxidation, as previously shown, but also MTP activity, Apo B lipidation into TG-rich VLDL particles, and hepatic lipoprotein secretion. Drugs with these dual effects may be more steatogenic than drugs acting only on β-oxidation or only MTP. (Hepatology 2003;38:133-140.)

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  • Inhibition of microsomal triglyceride transfer protein: Another mechanism for drug-induced steatosis in mice
    , 2003
    Co-Authors: Angela Sutton, Abdellah Mansouri, Bernard Fromenty, Dominique Pessayre

    Abstract:

    Although many steatogenic drugs inhibit mitochondrial fatty acid -oxidation, limited information is available on possible effects on hepatic lipoprotein secretion. In the endo-plasmic reticulum (ER) lumen, microsomal triglyceride transfer protein (MTP) lipidates apolipoprotein B (Apo B), to form triglyceride (TG)-rich very low density lipoprotein (VLDL) particles, which follow vesicular flow to the plasma membrane to be secreted, whereas incompletely lipidated Apo B particles are partly degraded. We studied hepatic MTP activity, the lipoproteins present in the ER lumen, and hepatic lipoprotein secretion 4 hours after administration of a single dose of Amineptine (1 mmol/kg), amiodarone (1 mmol/kg), doxycycline (0.25 mmol/kg), tetracycline (0.25 mmol/kg), tianeptine (0.5 mmol/ kg), or pirprofen (2 mmol/kg) in mice. These various doses have been shown previously to markedly inhibit fatty acid oxidation after a single dose, and to trigger steatosis either after repeated doses (doxycycline) or a single dose (other compounds) in mice. In the present study, Amineptine, amiodarone, pirprofen, tetracycline, and tianeptine, but not doxycycline, inhibited MTP activity in vitro, decreased ex vivo MTP activity in the hepatic homogenate of treated mice, decreased TG in the luminal VLDL fraction of hepatic microsomes of treate

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Herrera E Ceballos – One of the best experts on this subject based on the ideXlab platform.

  • acneiform eruption caused by Amineptine a case report and review of the literature
    Journal of The European Academy of Dermatology and Venereology, 2001
    Co-Authors: M V De Galvez Aranda, Sanchez P Sanchez, M Alonso J Corral, R Bosch J Garcia, M A Gallardo, Herrera E Ceballos

    Abstract:

    Acne caused by Amineptine has always been described with typical characteristic clinical features, and the retentional and cutaneous lesions are dose related. We present a case of acne-like eruption due to Amineptine in a woman under treatment for chronic depression.

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R. Fanelli – One of the best experts on this subject based on the ideXlab platform.

  • Pharmacokinetics of Amineptine in man.
    European Journal of Drug Metabolism and Pharmacokinetics, 2016
    Co-Authors: C. Sbarra, M. G. Castelli, A Noseda, R. Fanelli

    Abstract:

    The pharmacokinetics of the new stimulant agent Amineptine has been studied after its oral administration to healthy volunteers. No Statistically significant differences in pharmacokinetic parameters were observed when the drug was administered as capsules or tablets. The pharmacokinetic parameters also showed no change, after a 10-day course of repeated treatment with the drug.

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