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Peripheral Mechanisms of Mammalian Sweet Taste
Published in Robert H. Cagan, Neural Mechanisms in Taste, 2020
William Jakinovich, Dorothy Sugarman
In two-bottle preference experiments where various concentrations were tested, sodium cyclamate was uniformly rejected at all concentrations by pigs101 and rats,150,151 whereas in a mouse study, 1% sodium cyclamate was preferred to water, while higher concentrations were rejected.152 These results may have been due to the mouse’s preference for NaCl or the sodium cyclamate could have tasted like sucrose to the animal. In similar experiments using only single concentrations of sodium cyclamate, the cat,84 macaque monkey,135 and hamster121 treated this compound indifferently. The results of the hamster experiment were interpreted to suggest that sodium cyclamate is tasteless. However, the CTA results of Nowlis et al.81 suggest that sodium cyclamate tastes like sucrose and NaCl to the hamster. This apparent contradiction between preference and CTA conclusions reveals the weakness of the preference experiment and the need for further studies of the cyclamate taste response.
Quantitative structure–activity relationship models for compounds with anticonvulsant activity
Published in Expert Opinion on Drug Discovery, 2019
Carolina L. Bellera, Alan Talevi
The discriminant function was initially used to screen Merck Index database, discovering the anticonvulsants effects of abietic acid [76], preservatives methyl and propylparaben [51] and the artificial sweeteners acesulfame and sodium cyclamate [77]. Particular attention was given to food and medication additives since it was argued that they present well-characterized short- and long-term toxicity profiles. Regarding artificial sweeteners with anticonvulsant effects, it was hypothesized based on bioinformatic analysis that they might be targeting metabotropic glutamate receptors in the brain [75], although such hypothesis was not challenged experimentally. A subsequent article from the same group proved that sodium cyclamate is an nM inhibitor of carbonic anhydrase isoform VII, which has been proposed as an AED target [78].
Retail Availability and Characteristics of Addictive Areca Nut Products in a US Metropolis
Published in Journal of Psychoactive Drugs, 2021
Numerous sweeteners were listed on the purchased products, including saccharin, sugar, and interestingly sodium cyclamate, which currently is a banned substance by the Food and Drug Administration (FDA) (Beardsley 1984). In some cases, a generic designation of “sweetener” or “artificial sweetener” or “non-nutritive (N.N.) artificial sweetener” was stated instead of mentioning specific ingredient(s), so these products may also contain sodium cyclamate. Menthol was an additive found in many products labeled as mouth fresheners – this is interesting because menthol is known to enhance the psychosomatic effects of other drugs of abuse (e.g., nicotine) through inhibition of liver metabolism and pharmacodynamic adaptations of CNS nicotinic receptors (Alsharari et al. 2015).
A structure-based approach towards the identification of novel antichagasic compounds: Trypanosoma cruzi carbonic anhydrase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Manuel A. Llanos, María L. Sbaraglini, María L. Villalba, María D. Ruiz, Carolina Carrillo, Catalina Alba Soto, Alan Talevi, Andrea Angeli, Seppo Parkkila, Claudiu T. Supuran, Luciana Gavernet
Regarding the interaction with TcCA, most of the structures showed interesting inhibitory effect against the enzyme, with KI values in the nanomolar range. These results evidence the predictive capacity of the docking model to identify TcCA inhibitors. Particularly, sulphamide 5 is the most potent inhibitor of the set, with a KI value of 0.26 μM. Sodium cyclamate, a widely used sweetener, showed to be a potent TcCA inhibitor too. Concerning selectivity, both compounds are about 30 times more active against the parasite target than the human CA II, which represent an important aspect to be considered in future investigations.