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Chemosensory Influences on Eating and Drinking, and Their Cognitive Mediation
Published in Alan R. Hirsch, Nutrition and Sensation, 2023
There are indeed very few materials that laboratory rats can be reliably induced to ingest without food deprivation. Even the single complete food on which they are brought up and maintained is eaten in very variable small amounts unless it has been withheld for several hours (Le Magnen and Tallon 1966). Rats will drink strong solutions of salt when they are in sodium deficit but not otherwise. Only a very sweet solution of saccharin is consumed reliably on first access by an unfasted rat. Hence, the volume consumed of a novel saccharin solution was and still is used to measure the conditioning of aversion by association with poisoning or unfamiliar drug effects (Garcia, Kimeldorf, and Koelling 1955; Massei and Cowan 2002; Verendeev and Riley 2012). Saccharin has been mixed with sour or bitter agents in order to suppress its intake sufficiently for nutrient-conditioned preferences to be seen (Pain and Booth 1968; Booth and Davis 1973).
Peripheral Mechanisms of Mammalian Sweet Taste
Published in Robert H. Cagan, Neural Mechanisms in Taste, 2020
William Jakinovich, Dorothy Sugarman
The state of ionization of the saccharin molecule has been determined to be an important factor. Some investigators3,109 believe that saccharin is un-ionized when it stimulates the taste receptors, a view not shared by everyone.18,78,110 Perhaps the difference of opinion arises from an incorrectly published saccharin pK value of 11.68 in some editions of the Handbook of Chemistry.111 Earlier editions,112 as well as the published literature,113,114 have reported this value to be within the range of 1.6 to 2.32, which is in agreement with the strong acidic property of H-saccharin.
Carbohydrates
Published in Geoffrey P. Webb, Nutrition, 2019
Saccharin is 300–400 times sweeter than sugar and was the first artificial sweetener and has been in use since about 1880. Saccharin is absorbed and excreted unchanged in the urine. A study in the 1970s suggested that very large intakes increased the incidence of bladder tumours in male rats. Despite this, saccharin remained in use in most countries including the USA and the UK although it was banned for some years in Canada. Detailed risk evaluations suggest that the studies in male rats do not indicate any likely harm for people and that at practical intake levels it does not represent a hazard to human health and specifically does not increase cancer risk. Saccharin has a bitter aftertaste and is heat stable enough to be used as a sweetener in cooking although only tiny amounts are used.
Consumption patterns of nonnutritive sweeteners among university students at a Caribbean institution
Published in Journal of American College Health, 2021
Marquitta C. Webb, Dana Chong, Sa’eed Bawa
Less than one quarter of university students indicated that NNS cause cancer. This may be due to a lack of education on the health benefits and/or risks associated with the use of these NNS. In a systematic literature review,30 researchers examined 41 case-control studies which assessed the effect of NNS on cancer (i.e. bladder cancer and urinary tract cancer) and found mixed results. Out of the 41 studies, 11 describe a positive association between artificial/NNS and bladder cancer and urinary tract cancer. However, 20 report no association.30 In the early 1970, the NNS, saccharin in combination with cyclamate were linked to bladder cancer in laboratory animals. It is important to note that the results obtain from mechanistic studies indicate that this problem only apply to rats and not humans. Further, reports from subsequent carcinogenicity and human epidemiology studies showed no consistent evidence that saccharin is associated with bladder cancer incidence.35
Gabapentin–saccharin co-crystals with enhanced physicochemical properties and in vivo absorption formulated as oro-dispersible tablets
Published in Pharmaceutical Development and Technology, 2020
Iman I. Soliman, Soha M. Kandil, Ebtsam M. Abdou
Bitterness scores for different Gaba tablet preparations showed the ability of sacch to improve the bitter taste of Gaba either when it was used as a physical mixture or as a coformer in the cocrystals with some advantages for the cocrystals over the physical mixture, Table 3. It is known that saccharin is widely used artificial safe sweetening agent which is five hundred times sweeter than sugar and it is used for masking of the bitter taste especially in pediatric and diabetic patients due to its non-glycogenic characteristic (Tayebi and Mortazavi 2011). Moreover, mannitol has been reported to enhance mouth feel as it produces cooling sensation due to its negative heat of solution (Shinde et al. 2010; Kalyankar et al. 2015). Slightly higher improvement of the taste was obtained with tablets formulated with Gaba-sacch cocrystals due to the effect of cocrystallization which have been claimed to be potential alternative for masking the bitter taste of the drugs (Aitipamula et al. 2018). It is worthy here to mention that both the two tablet formulations exhibited bitter aftertaste action due to the inherent bitter aftertaste of the sweetener saccharin.
New sulfonamides containing organometallic-acylhydrazones: synthesis, characterisation and biological evaluation as inhibitors of human carbonic anhydrases
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Yosselin Huentupil, Luis Peña, Néstor Novoa, Emanuela Berrino, Rodrigo Arancibia, Claudiu T. Supuran
Carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) are clinically used for several decades as diuretics1, antiglaucoma agents2, antiobesity drugs3, and more recently, a number of studies showed that CA inhibition has profound antitumor effects by inhibition of hypoxia-inducible isoforms CA IX and XII, overexpressed in many hypoxic tumors4. Several proof-of-concept studies demonstrated the involvement of some CA isoforms in neuropathic pain5 and arthritis6, with inhibitors of the sulfonamide/coumarin7 types demonstrating significant effects in vivo, in animal models of these diseases. This is obviously due to the fact that at least 15 different α-class CA isoforms are present in humans, and many of them are drug targets for the treatment or prevention of this large variety of pathologies1–7. Thus, the field of drug design, synthesis and in vivo investigations of various types of CAIs is a highly dynamic one, with a large number of interesting new chemotypes acting on these widespread enzymes constantly emerging1–7. Among the clinically used sulfonamide CAIs are acetazolamide (AAZ), methazolamide (MZA), ethoxzolamide (EZA), brinzolamide (BRZ) and dorzolamide (DRZ) – (Figure 1)1–3. Saccharin (SAC) is a sweetener widely used in beverages and food1–3.