The Experts below are selected from a list of 264 Experts worldwide ranked by ideXlab platform
Neil E. Rowland - One of the best experts on this subject based on the ideXlab platform.
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effect of serotonergic Anorectics on food intake and induction of fos in brain of mice with disruption of melanocortin 3 and or 4 receptors
Pharmacology Biochemistry and Behavior, 2010Co-Authors: Neil E. Rowland, Kaihan Fakhar, Kimberly L Robertson, Carrie HaskellluevanoAbstract:Previous studies have indicated that type 3 or 4 melanocortin receptors (MCR) are downstream of the critical anorectic action of drugs that stimulate 5-HT2C receptors. To characterize further the receptor types involved, we have studied the effect of serotonergic Anorectics in mice with genomic disruption of either MC3R or MC4R, or their combined knockout. In a first experiment, we showed that wild type (WT) and MC4R−/− mice showed comparable inhibition of food intake following acute treatment with dexnorfenfluramine. In a second experiment using WAY-161503, a 5-HT receptor full agonist with selectivity for 2B and 2C subtypes, we found that MC4R−/− responded comparably to WT, while MC3R−/− had reduced sensitivity. Double receptor knockout (DKO) mice responded comparably to WT and MC4R−/−. Surprisingly, brain Fos-ir was not strongly induced in any brain region by WAY-16103 with the exception of the paraventricular nucleus of DKO. These data suggest that MC3Rs may be involved in the response to serotonergic anorectic agents, and more generally in control of food intake.
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anorectic efficacy of the fenfluramine phentermine combination in rats additivity or synergy
European Journal of Pharmacology, 1999Co-Authors: Jonathan D Roth, Neil E. RowlandAbstract:Fenfluramine + phentermine was a widely used combination for weight loss. Fenfluramine and phentermine are believed to act via serotonin and catecholamines, respectively. To what extent these drugs interact has not been well-established. We compared the anorectic efficacy of a range of doses of the combination (using dexfenfluramine instead of fenfluramine) relative to a range of doses of the individual drugs in 90 min sweetened milk intake tests in deprived and nondeprived rats. Results were plotted on isobolograms to determine whether the anorectic effects of the combination were either additive or synergistic. Collectively, the isobolographic analysis revealed that: (1) under acute conditions, dexfenfluramine and phentermine interact for the most part in a synergistic manner, and (2) with the exception of phentermine alone, deprivation state at time of testing did not alter the efficacy of the Anorectics. These findings suggest that combined drug treatment for obesity is a theoretical approach that merits further investigation.
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Anorectic efficacy of the fenfluramine/phentermine combination in rats : additivity or synergy?
European Journal of Pharmacology, 1999Co-Authors: Jonathan D Roth, Neil E. RowlandAbstract:Fenfluramine + phentermine was a widely used combination for weight loss. Fenfluramine and phentermine are believed to act via serotonin and catecholamines, respectively. To what extent these drugs interact has not been well-established. We compared the anorectic efficacy of a range of doses of the combination (using dexfenfluramine instead of fenfluramine) relative to a range of doses of the individual drugs in 90 min sweetened milk intake tests in deprived and nondeprived rats. Results were plotted on isobolograms to determine whether the anorectic effects of the combination were either additive or synergistic. Collectively, the isobolographic analysis revealed that: (1) under acute conditions, dexfenfluramine and phentermine interact for the most part in a synergistic manner, and (2) with the exception of phentermine alone, deprivation state at time of testing did not alter the efficacy of the Anorectics. These findings suggest that combined drug treatment for obesity is a theoretical approach that merits further investigation.
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efficacy of administration of dexfenfluramine and phentermine alone and in combination on ingestive behavior and body weight in rats
Psychopharmacology, 1998Co-Authors: Jonathan D Roth, Neil E. RowlandAbstract:Recently, a combination of the Anorectics fenfluramine (FEN) and phentermine (PHEN) has been used to treat obesity. While each of these agents has been investigated in animals, little is known concerning the effects of the combination on ingestive behavior and body weight. In the present experiments, we report: (1) the effects of acute administration of dexfenfluramine (DFEN) and PHEN individually and in combination on sweetened milk intake and body weight in non-deprived rats and (2) the effects of chronic administration (7 day minipump) of DFEN, PHEN, and their combination on daily food intake and body weight both during and after the treatment period. Additionally, the effects of the 5-HT2C agonist 1-[3-(trifluoromethyl)-phenyl]piperazine (TFMPP) alone and in combination with PHEN on food intake and body weight were assessed. Both acute and chronic administration of DFEN and PHEN revealed that in combination they are more effective than when given individually. However, the DFEN/ PHEN combination does not appear to exert effects that are selective for food intake because water intake was markedly suppressed in water-deprived rats. PHEN alone or in combination with either DFEN or TFMPP also produced increased activity or alertness during the day when controls normally were asleep. While anorectic combinations such as DFEN/PHEN may be effective at promoting weight loss and reducing food intake, future studies on their specificity, safety and efficacy are warranted.
Maria De La Paz Aguilar-caballos - One of the best experts on this subject based on the ideXlab platform.
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Counterfeit formulations: analytical perspective on Anorectics
Forensic Toxicology, 2021Co-Authors: Dan Osei Mensah Bonsu, Constance Afoakwah, Maria De La Paz Aguilar-caballosAbstract:This paper examines the scope of Anorectics in counterfeit weight-reducing formulations and provides insight into the present state of research in determining such adulterants. Analytical techniques utilised in profiling adulterants found in slimming products, including limitations and mitigation steps of these conventional methods are also discussed. The current legal status of the Anorectics and analogues routinely encountered in non-prescription slimming formulations is also explored. All reviewed literature was extracted from Scopus, Web of Science, PubMed, and Google Scholar databases using relevant search terms, such as, ‘counterfeit drugs’, ‘weight loss drugs’, ‘weight-reducing drugs’, ‘slimming drugs’, ‘anorectic agents’, and ‘counterfeit anorexics’. Legislation related to Anorectics was obtained from the portals of various government and international agencies. Anorectics frequently profiled in counterfeit slimming formulations are mostly amphetamine derivatives or its analogues. Five routinely reported pharmacological classes of adulterants, namely anxiolytics, diuretics, antidepressants, laxatives, and stimulants, are mainly utilised as coadjuvants in fake weigh-reducing formulations to increase bioavailability or to minimise anticipated side effects. Liquid and gas chromatography coupled with mass spectrometric detectors are predominantly used techniques for anorectic analysis due to the possibility of obtaining detailed information of adulterants. However, interference from the complex sample matrices of these fake products limits the accuracy of these methods and requires robust sample preparation methods for enhanced sensitivity and selectivity. The most common Anorectics found in counterfeit slimming medicines are either completely banned or available by prescription only, in many countries. Slimming formulations doped with anorectic cocktails to boost their weight-reducing efficacy are not uncommon. Liquid chromatography combined with mass spectrometry remains the gold standard for counterfeit drug analysis, and requires improved preconcentration methods for rapid and quantitative identification of specific chemical constituents. Extensive method development and validation, targeted at refining existing techniques while developing new ones, is expected to improve the analytical profiling of counterfeit Anorectics significantly.
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Counterfeit formulations: analytical perspective on Anorectics
Forensic Toxicology, 2021Co-Authors: Dan Osei Mensah Bonsu, Constance Afoakwah, Maria De La Paz Aguilar-caballosAbstract:Purpose This paper examines the scope of Anorectics in counterfeit weight-reducing formulations and provides insight into the present state of research in determining such adulterants. Analytical techniques utilised in profiling adulterants found in slimming products, including limitations and mitigation steps of these conventional methods are also discussed. The current legal status of the Anorectics and analogues routinely encountered in non-prescription slimming formulations is also explored. Methods All reviewed literature was extracted from Scopus, Web of Science, PubMed, and Google Scholar databases using relevant search terms, such as, ‘counterfeit drugs’, ‘weight loss drugs’, ‘weight-reducing drugs’, ‘slimming drugs’, ‘anorectic agents’, and ‘counterfeit anorexics’. Legislation related to Anorectics was obtained from the portals of various government and international agencies. Results Anorectics frequently profiled in counterfeit slimming formulations are mostly amphetamine derivatives or its analogues. Five routinely reported pharmacological classes of adulterants, namely anxiolytics, diuretics, antidepressants, laxatives, and stimulants, are mainly utilised as coadjuvants in fake weigh-reducing formulations to increase bioavailability or to minimise anticipated side effects. Liquid and gas chromatography coupled with mass spectrometric detectors are predominantly used techniques for anorectic analysis due to the possibility of obtaining detailed information of adulterants. However, interference from the complex sample matrices of these fake products limits the accuracy of these methods and requires robust sample preparation methods for enhanced sensitivity and selectivity. The most common Anorectics found in counterfeit slimming medicines are either completely banned or available by prescription only, in many countries. Conclusions Slimming formulations doped with anorectic cocktails to boost their weight-reducing efficacy are not uncommon. Liquid chromatography combined with mass spectrometry remains the gold standard for counterfeit drug analysis, and requires improved preconcentration methods for rapid and quantitative identification of specific chemical constituents. Extensive method development and validation, targeted at refining existing techniques while developing new ones, is expected to improve the analytical profiling of counterfeit Anorectics significantly.
Angela Uslenghi - One of the best experts on this subject based on the ideXlab platform.
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Comparative studies on the anorectic activity of d-fenfluramine in mice, rats, and guinea pigs
Naunyn-Schmiedeberg's Archives of Pharmacology, 1991Co-Authors: Tiziana Mennini, Adalgisa Bizzi, Silvio Caccia, Annamaria Codegoni, Claudia Fracasso, Emanuela Frittoli, Giovanna Guiso, Ines Martin Padura, Carlo Taddei, Angela UslenghiAbstract:The present study compares the anorectic activity of d -fenfluramine and its metabolite d -norfenfluramine in three animal species. d -Fenfluramine and d -norfenfluramine show anorectic activity at increasing doses (ED_50) in rats, guinea pigs, and mice, d -norfenfluramine being more active than d -fenfluramine in all three species. Equiactive anorectic activities are reached with different brain levels of d -fenfluramine and d -norfenfluramine, guinea pigs being the most sensitive species, followed by rats then mice. The metabolite most probably plays a major role in the anorectic effect of d -fenfluramine in guinea pigs, contributes to the anorectic activity in rats, but adds little to the action of the parent drug in mice. The different sensitivity to d -fenfluramine and d -norfenfluramine in these three species does not appear to be explained by a number of biochemical parameters, including serotonin uptake or release, receptor subtypes, or ^3H- d -fenfluramine binding and uptake.
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Comparative studies on the anorectic activity of d-fenfluramine in mice, rats, and guinea pigs
Naunyn-Schmiedeberg's Archives of Pharmacology, 1991Co-Authors: Tiziana Mennini, Adalgisa Bizzi, Silvio Caccia, Annamaria Codegoni, Claudia Fracasso, Emanuela Frittoli, Giovanna Guiso, Ines Martin Padura, Carlo Taddei, Angela UslenghiAbstract:The present study compares the anorectic activity of d -fenfluramine and its metabolite d -norfenfluramine in three animal species. d -Fenfluramine and d -norfenfluramine show anorectic activity at increasing doses (ED_50) in rats, guinea pigs, and mice, d -norfenfluramine being more active than d -fenfluramine in all three species. Equiactive anorectic activities are reached with different brain levels of d -fenfluramine and d -norfenfluramine, guinea pigs being the most sensitive species, followed by rats then mice. The metabolite most probably plays a major role in the anorectic effect of d -fenfluramine in guinea pigs, contributes to the anorectic activity in rats, but adds little to the action of the parent drug in mice. The different sensitivity to d -fenfluramine and d -norfenfluramine in these three species does not appear to be explained by a number of biochemical parameters, including serotonin uptake or release, receptor subtypes, or ^3H- d -fenfluramine binding and uptake.
Jonathan D Roth - One of the best experts on this subject based on the ideXlab platform.
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anorectic efficacy of the fenfluramine phentermine combination in rats additivity or synergy
European Journal of Pharmacology, 1999Co-Authors: Jonathan D Roth, Neil E. RowlandAbstract:Fenfluramine + phentermine was a widely used combination for weight loss. Fenfluramine and phentermine are believed to act via serotonin and catecholamines, respectively. To what extent these drugs interact has not been well-established. We compared the anorectic efficacy of a range of doses of the combination (using dexfenfluramine instead of fenfluramine) relative to a range of doses of the individual drugs in 90 min sweetened milk intake tests in deprived and nondeprived rats. Results were plotted on isobolograms to determine whether the anorectic effects of the combination were either additive or synergistic. Collectively, the isobolographic analysis revealed that: (1) under acute conditions, dexfenfluramine and phentermine interact for the most part in a synergistic manner, and (2) with the exception of phentermine alone, deprivation state at time of testing did not alter the efficacy of the Anorectics. These findings suggest that combined drug treatment for obesity is a theoretical approach that merits further investigation.
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Anorectic efficacy of the fenfluramine/phentermine combination in rats : additivity or synergy?
European Journal of Pharmacology, 1999Co-Authors: Jonathan D Roth, Neil E. RowlandAbstract:Fenfluramine + phentermine was a widely used combination for weight loss. Fenfluramine and phentermine are believed to act via serotonin and catecholamines, respectively. To what extent these drugs interact has not been well-established. We compared the anorectic efficacy of a range of doses of the combination (using dexfenfluramine instead of fenfluramine) relative to a range of doses of the individual drugs in 90 min sweetened milk intake tests in deprived and nondeprived rats. Results were plotted on isobolograms to determine whether the anorectic effects of the combination were either additive or synergistic. Collectively, the isobolographic analysis revealed that: (1) under acute conditions, dexfenfluramine and phentermine interact for the most part in a synergistic manner, and (2) with the exception of phentermine alone, deprivation state at time of testing did not alter the efficacy of the Anorectics. These findings suggest that combined drug treatment for obesity is a theoretical approach that merits further investigation.
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efficacy of administration of dexfenfluramine and phentermine alone and in combination on ingestive behavior and body weight in rats
Psychopharmacology, 1998Co-Authors: Jonathan D Roth, Neil E. RowlandAbstract:Recently, a combination of the Anorectics fenfluramine (FEN) and phentermine (PHEN) has been used to treat obesity. While each of these agents has been investigated in animals, little is known concerning the effects of the combination on ingestive behavior and body weight. In the present experiments, we report: (1) the effects of acute administration of dexfenfluramine (DFEN) and PHEN individually and in combination on sweetened milk intake and body weight in non-deprived rats and (2) the effects of chronic administration (7 day minipump) of DFEN, PHEN, and their combination on daily food intake and body weight both during and after the treatment period. Additionally, the effects of the 5-HT2C agonist 1-[3-(trifluoromethyl)-phenyl]piperazine (TFMPP) alone and in combination with PHEN on food intake and body weight were assessed. Both acute and chronic administration of DFEN and PHEN revealed that in combination they are more effective than when given individually. However, the DFEN/ PHEN combination does not appear to exert effects that are selective for food intake because water intake was markedly suppressed in water-deprived rats. PHEN alone or in combination with either DFEN or TFMPP also produced increased activity or alertness during the day when controls normally were asleep. While anorectic combinations such as DFEN/PHEN may be effective at promoting weight loss and reducing food intake, future studies on their specificity, safety and efficacy are warranted.
Dan Osei Mensah Bonsu - One of the best experts on this subject based on the ideXlab platform.
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Counterfeit formulations: analytical perspective on Anorectics
Forensic Toxicology, 2021Co-Authors: Dan Osei Mensah Bonsu, Constance Afoakwah, Maria De La Paz Aguilar-caballosAbstract:This paper examines the scope of Anorectics in counterfeit weight-reducing formulations and provides insight into the present state of research in determining such adulterants. Analytical techniques utilised in profiling adulterants found in slimming products, including limitations and mitigation steps of these conventional methods are also discussed. The current legal status of the Anorectics and analogues routinely encountered in non-prescription slimming formulations is also explored. All reviewed literature was extracted from Scopus, Web of Science, PubMed, and Google Scholar databases using relevant search terms, such as, ‘counterfeit drugs’, ‘weight loss drugs’, ‘weight-reducing drugs’, ‘slimming drugs’, ‘anorectic agents’, and ‘counterfeit anorexics’. Legislation related to Anorectics was obtained from the portals of various government and international agencies. Anorectics frequently profiled in counterfeit slimming formulations are mostly amphetamine derivatives or its analogues. Five routinely reported pharmacological classes of adulterants, namely anxiolytics, diuretics, antidepressants, laxatives, and stimulants, are mainly utilised as coadjuvants in fake weigh-reducing formulations to increase bioavailability or to minimise anticipated side effects. Liquid and gas chromatography coupled with mass spectrometric detectors are predominantly used techniques for anorectic analysis due to the possibility of obtaining detailed information of adulterants. However, interference from the complex sample matrices of these fake products limits the accuracy of these methods and requires robust sample preparation methods for enhanced sensitivity and selectivity. The most common Anorectics found in counterfeit slimming medicines are either completely banned or available by prescription only, in many countries. Slimming formulations doped with anorectic cocktails to boost their weight-reducing efficacy are not uncommon. Liquid chromatography combined with mass spectrometry remains the gold standard for counterfeit drug analysis, and requires improved preconcentration methods for rapid and quantitative identification of specific chemical constituents. Extensive method development and validation, targeted at refining existing techniques while developing new ones, is expected to improve the analytical profiling of counterfeit Anorectics significantly.
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Counterfeit formulations: analytical perspective on Anorectics
Forensic Toxicology, 2021Co-Authors: Dan Osei Mensah Bonsu, Constance Afoakwah, Maria De La Paz Aguilar-caballosAbstract:Purpose This paper examines the scope of Anorectics in counterfeit weight-reducing formulations and provides insight into the present state of research in determining such adulterants. Analytical techniques utilised in profiling adulterants found in slimming products, including limitations and mitigation steps of these conventional methods are also discussed. The current legal status of the Anorectics and analogues routinely encountered in non-prescription slimming formulations is also explored. Methods All reviewed literature was extracted from Scopus, Web of Science, PubMed, and Google Scholar databases using relevant search terms, such as, ‘counterfeit drugs’, ‘weight loss drugs’, ‘weight-reducing drugs’, ‘slimming drugs’, ‘anorectic agents’, and ‘counterfeit anorexics’. Legislation related to Anorectics was obtained from the portals of various government and international agencies. Results Anorectics frequently profiled in counterfeit slimming formulations are mostly amphetamine derivatives or its analogues. Five routinely reported pharmacological classes of adulterants, namely anxiolytics, diuretics, antidepressants, laxatives, and stimulants, are mainly utilised as coadjuvants in fake weigh-reducing formulations to increase bioavailability or to minimise anticipated side effects. Liquid and gas chromatography coupled with mass spectrometric detectors are predominantly used techniques for anorectic analysis due to the possibility of obtaining detailed information of adulterants. However, interference from the complex sample matrices of these fake products limits the accuracy of these methods and requires robust sample preparation methods for enhanced sensitivity and selectivity. The most common Anorectics found in counterfeit slimming medicines are either completely banned or available by prescription only, in many countries. Conclusions Slimming formulations doped with anorectic cocktails to boost their weight-reducing efficacy are not uncommon. Liquid chromatography combined with mass spectrometry remains the gold standard for counterfeit drug analysis, and requires improved preconcentration methods for rapid and quantitative identification of specific chemical constituents. Extensive method development and validation, targeted at refining existing techniques while developing new ones, is expected to improve the analytical profiling of counterfeit Anorectics significantly.