Details
Stereochemistry | ACHIRAL |
Molecular Formula | C7H4NO3S.Na.2H2O |
Molecular Weight | 241.197 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.O.[Na+].O=C1[N-]S(=O)(=O)C2=C1C=CC=C2
InChI
InChIKey=AYGJDUHQRFKLBG-UHFFFAOYSA-M
InChI=1S/C7H5NO3S.Na.2H2O/c9-7-5-3-1-2-4-6(5)12(10,11)8-7;;;/h1-4H,(H,8,9);;2*1H2/q;+1;;/p-1
DescriptionSources: https://www.cancer.gov/about-cancer/causes-prevention/risk/diet/artificial-sweeteners-fact-sheetCurator's Comment: description was created based on several sources, including
http://www.diabetes.co.uk/sweeteners/saccharin.html
http://www.ukfoodguide.net/e954.htm
Sources: https://www.cancer.gov/about-cancer/causes-prevention/risk/diet/artificial-sweeteners-fact-sheet
Curator's Comment: description was created based on several sources, including
http://www.diabetes.co.uk/sweeteners/saccharin.html
http://www.ukfoodguide.net/e954.htm
Saccharin is the most established of the artificial sweeteners on the market, this mixture of dextrose and saccharin has been in use for over a century and is found in diet versions of soft drinks. It is 300-500 times sweeter than sugar and contains zero calories. In 1977, the FDA tried to ban its use after evidence showed it caused cancer in rats. Extensive lobbying by the diet food industry allowed products to stay on the shelves as long as they carried warnings about the cancer risks in animals. This warning was removed in 2001 when the Calorie Control Council insisted the link between animal and human cancers could not automatically be made. Consumption of saccharin-sweetened products can benefit diabetics as the substance goes directly through the human digestive system without being digested. While saccharin has no food energy, it can trigger the release of insulin in humans due to its sweet taste. The T1R2/R3 sweet taste receptor exist on the surface of pancreatic beta cells. Saccharin is a unique in that it inhibits glucose-stimulated insulin secretion (GSIS) at submaximal and maximal glucose concentrations, with the other sweeteners having no effect. Investigation of saccharin’s dose-response characteristics showed that concentrations of 0.1 and 0.5 mM stimulated insulin secretion, while concentrations of 1 and 2.5 mM inhibited insulin secretion. Saccharin’s effect on insulin secretion was shown to be reversible in INS-1 832/13 clonal pancreatic beta cells after chronic exposure to 1 mM saccharin. Artificial sweeteners may affect insulin secretion via interaction with the sweet taste receptor, also saccharin may affect other cellular processes linked to insulin secretion, and that these effects are both time- and concentration-dependent
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: Q8TE23 Gene ID: 80834.0 Gene Symbol: TAS1R2 Target Organism: Homo sapiens (Human) Sources: http://www.fasebj.org/content/25/1_Supplement/530.1 |
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Target ID: Q7RTX0 Gene ID: 83756.0 Gene Symbol: TAS1R3 Target Organism: Homo sapiens (Human) Sources: http://www.fasebj.org/content/25/1_Supplement/530.1 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Cmax
Value | Dose | Co-administered | Analyte | Population |
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14 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/ |
2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered: |
SACCHARIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
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27 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/ |
2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered: |
SACCHARIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
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5800 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/ |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: PROBENECID |
SACCHARIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
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3700 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/ |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
SACCHARIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6500 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/ |
2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered: |
SACCHARIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
6800 μg × min/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7303723/ |
2 g single, oral dose: 2 g route of administration: Oral experiment type: SINGLE co-administered: |
SACCHARIN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
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Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
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no | no (co-administration study) Comment: coadministration with bupropion: had no effect on the CYP2B activity |
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no | no (co-administration study) Comment: coadministration with bupropion: saccharin had no inhibitory effect on CYP2B activity in vivo |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
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no |
PubMed
Title | Date | PubMed |
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Elevated expression of glucose transporter-1 in hypothalamic ependymal cells not involved in the formation of the brain-cerebrospinal fluid barrier. | 2001 |
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Serial changes in 14C-deoxyglucose and 201Tl uptake in autoimmune myocarditis in rats. | 2001 Feb |
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Na+-to-sugar stoichiometry of SGLT3. | 2001 Feb |
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Golgi complex, endoplasmic reticulum exit sites, and microtubules in skeletal muscle fibers are organized by patterned activity. | 2001 Feb 1 |
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Anti-tumor immunity provided by a synthetic multiple antigenic glycopeptide displaying a tri-Tn glycotope. | 2001 Feb 15 |
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GLUT4--at the cross roads between membrane trafficking and signal transduction. | 2001 Jan |
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Suppression of ethanol responding by centrally administered CTOP and naltrindole in AA and Wistar rats. | 2001 Jan |
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What's the truth about the health risks of sugar substitutes such as saccharin and aspartame? | 2001 Jan |
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The rate-limiting step for tumor [18F]fluoro-2-deoxy-D-glucose (FDG) incorporation. | 2001 Jan |
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High-resolution genetic mapping of the saccharin preference locus (Sac) and the putative sweet taste receptor (T1R1) gene (Gpr70) to mouse distal Chromosome 4. | 2001 Jan |
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Improved diabetic syndrome in C57BL/KsJ-db/db mice by oral administration of the Na(+)-glucose cotransporter inhibitor T-1095. | 2001 Jan |
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The synaptic vesicle protein, cysteine-string protein, is associated with the plasma membrane in 3T3-L1 adipocytes and interacts with syntaxin 4. | 2001 Jan |
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Expression of auxilin or AP180 inhibits endocytosis by mislocalizing clathrin: evidence for formation of nascent pits containing AP1 or AP2 but not clathrin. | 2001 Jan |
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Developmental reprogramming of rat GLUT-5 requires de novo mRNA and protein synthesis. | 2001 Jan |
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Cellular responses of NG108-15 and SK-N-MC lines to sweet and bitter tastants as measured by extracellular acidification rates. | 2001 Jan 1 |
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Motivational effects of ethanol in DARPP-32 knock-out mice. | 2001 Jan 1 |
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Polysaccharides of green Arabica and Robusta coffee beans. | 2001 Jan 15 |
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Engineering conformational flexibility in the lactose permease of Escherichia coli: use of glycine-scanning mutagenesis to rescue mutant Glu325-->Asp. | 2001 Jan 23 |
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Genetic multiplicity of the human UDP-glucuronosyltransferases and regulation in the gastrointestinal tract. | 2001 Mar |
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Hormonal regulation of chicken intestinal NHE and SGLT-1 activities. | 2001 Mar |
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Model of the 3-D structure of the GLUT3 glucose transporter and molecular dynamics simulation of glucose transport. | 2001 Mar 1 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://en.foodlexicon.org/s0001100.php
no more than 80 to 3000 mg saccharin per kilogram or litre should be used
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/3928589
After assaying for prolactin (PRL) in saccharin-treated cultures, it was observed that this sweetener is also capable of stimulating PRL production two- to sixfold in a dose-dependent manner. Enhancement of PRL production can be observed at 0.5 mM saccharin, yet this is 10 times less than the saccharin concentration required to alter cell shape. These effects of saccharin on cell morphology and on PRL production are reversible in rat pituitary tumor cells (GH4C1). When added to cultures along with maximal concentrations of epidermal growth factor (EGF) or thyrotropin-releasing hormone (TRH), the effects of saccharin on PRL production are additive, suggesting that the actions of saccharin are mediated by a somewhat different pathway from that of the peptide hormones
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Classification Tree | Code System | Code | ||
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CODEX ALIMENTARIUS (GSFA) |
INS-594(IV)
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JECFA EVALUATION |
INS-954(IV)
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NCI_THESAURUS |
C283
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281678
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C76516
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517320
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SACCHARIN SODIUM
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PRIMARY | Description: Colourless crystals or a white, crystalline powder; odourless or almost odourless. Solubility: Freely soluble in water; sparingly soluble in ethanol (~750 g/l) TS; practically insoluble in ether R. Category: Sweetening agent. Storage: Saccharin sodium should be kept in a well-closed container. Additional information: Saccharin sodium effloresces slowly in air and loses about half of its content of water of crystallization. It has a very sweet taste, even in very dilute solutions.Requirements: Saccharin sodium contains not less than 98.0% and not more than the equivalent of 101.0% of C7H4NNaO3S, calculated with reference to the anhydrous substance. | ||
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1607040
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ACTIVE MOIETY
SUBSTANCE RECORD