Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C7H4NO3S.Na |
| Molecular Weight | 205.166 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].O=C1[N-]S(=O)(=O)C2=C1C=CC=C2
InChI
InChIKey=WINXNKPZLFISPD-UHFFFAOYSA-M
InChI=1S/C7H5NO3S.Na/c9-7-5-3-1-2-4-6(5)12(10,11)8-7;/h1-4H,(H,8,9);/q;+1/p-1
| Molecular Formula | Na |
| Molecular Weight | 22.9898 |
| Charge | 1 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C7H5NO3S |
| Molecular Weight | 183.185 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q8TE23 Gene ID: 80834.0 Gene Symbol: TAS1R2 Target Organism: Homo sapiens (Human) |
|||
Target ID: Q7RTX0 Gene ID: 83756.0 Gene Symbol: TAS1R3 Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
|---|---|---|---|---|
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 |
|
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 |
|---|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| no | no (co-administration study) Comment: coadministration with bupropion: had no effect on the CYP2B activity |
|||
| 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 |
|---|---|---|---|---|
| no |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Cytological and lectin histochemical characterization of secretion production and secretion composition in the tubular glands of the canine anal sacs. | 2001 |
|
| A new type of endo-xyloglucan transferase devoted to xyloglucan hydrolysis in the cell wall of azuki bean epicotyls. | 2001 Feb |
|
| [Micelle-mediated extraction for concentrating conjugated bilirubin in urine]. | 2001 Feb |
|
| Serial changes in 14C-deoxyglucose and 201Tl uptake in autoimmune myocarditis in rats. | 2001 Feb |
|
| Na+-to-sugar stoichiometry of SGLT3. | 2001 Feb |
|
| Involvement of PI 3-kinase in IGF-I stimulation of jejunal Na+-K+-ATPase activity and nutrient absorption. | 2001 Feb |
|
| Diurnal rhythmicity in intestinal SGLT-1 function, V(max), and mRNA expression topography. | 2001 Feb |
|
| Automated noninvasive measurement of cyclophosphamide-induced changes in murine voiding frequency and volume. | 2001 Feb |
|
| Characterization of EDTA-soluble polysaccharides from the scape of Musa paradisiaca (banana). | 2001 Feb |
|
| Negative-ion electrospray mass spectrometry of neutral underivatized oligosaccharides. | 2001 Feb 1 |
|
| Skeletal muscle and insulin sensitivity: pathophysiological alterations. | 2001 Feb 1 |
|
| Cysteine residues in the D-galactose-H+ symport protein of Escherichia coli: effects of mutagenesis on transport, reaction with N-ethylmaleimide and antibiotic binding. | 2001 Feb 1 |
|
| Glucans exhibit weak antioxidant activity, but stimulate macrophage free radical activity. | 2001 Feb 15 |
|
| Adipose-selective targeting of the GLUT4 gene impairs insulin action in muscle and liver. | 2001 Feb 8 |
|
| Diabetes. Dialogue between muscle and fat. | 2001 Feb 8 |
|
| Further glucosides of lichens' acids from Central Asian lichens. | 2001 Jan |
|
| A novel assay method for glycosphingolipid deacylase by enzyme-linked immunochemical detection of lysoglycosphingolipid. | 2001 Jan |
|
| An overview of pathophysiology and treatment of insulin resistance. | 2001 Jan |
|
| GLUT4--at the cross roads between membrane trafficking and signal transduction. | 2001 Jan |
|
| Distinct long-term regulation of glycerol and non-esterified fatty acid release by insulin and TNF-alpha in 3T3-L1 adipocytes. | 2001 Jan |
|
| Distinct differences in binding capacity to saccharide epitopes in supratentorial pilocytic astrocytomas, astrocytomas, anaplastic astrocytomas, and glioblastomas. | 2001 Jan |
|
| Suppression of ethanol responding by centrally administered CTOP and naltrindole in AA and Wistar rats. | 2001 Jan |
|
| What's the truth about the health risks of sugar substitutes such as saccharin and aspartame? | 2001 Jan |
|
| Hypoxia-Induced increase in FDG uptake in MCF7 cells. | 2001 Jan |
|
| The Schistosoma mansoni host-interactive tegument forms from vesicle eruptions of a cyton network. | 2001 Jan |
|
| Changes of nasal function after temperature-controlled radiofrequency tissue volume reduction for the turbinate. | 2001 Jan |
|
| The rate-limiting step for tumor [18F]fluoro-2-deoxy-D-glucose (FDG) incorporation. | 2001 Jan |
|
| 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 |
|
| Placental glucose transport in gestational diabetes mellitus. | 2001 Jan |
|
| A saccharinate-iron(II) complex with a free saccharin molecule present, [Fe(phen)3]sac2.sacH.6H2O. | 2001 Jan |
|
| Improved water solubility of neohesperidin dihydrochalcone in sweetener blends. | 2001 Jan |
|
| Functional asymmetry of the sodium-D-glucose cotransporter expressed in yeast secretory vesicles. | 2001 Jan 15 |
|
| Polysaccharides of green Arabica and Robusta coffee beans. | 2001 Jan 15 |
|
| The occurrence of internal (1 --> 5)-linked arabinofuranose and arabinopyranose residues in arabinogalactan side chains from soybean pectic substances. | 2001 Jan 15 |
|
| Compositional analysis of glycosaminoglycans by electrospray mass spectrometry. | 2001 Jan 15 |
|
| Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors. | 2001 Jan 23 |
|
| Engineering conformational flexibility in the lactose permease of Escherichia coli: use of glycine-scanning mutagenesis to rescue mutant Glu325-->Asp. | 2001 Jan 23 |
|
| Identification of N- and O-linked oligosaccharides in human seminal vesicles. | 2001 Jan-Feb |
|
| Effect of growth hormone on intestinal Na+/glucose cotransporter activity. | 2001 Jan-Feb |
|
| Spatial compartmentalization of signal transduction in insulin action. | 2001 Mar |
|
| Development of cataractous macrophthalmia in mice expressing an active MEK1 in the lens. | 2001 Mar |
|
| Time-resolved study of the inner space of lactose permease. | 2001 Mar |
|
| Effects of excitotoxic brain lesions on taste-mediated odor learning in the rat. | 2001 Mar |
|
| Genetic multiplicity of the human UDP-glucuronosyltransferases and regulation in the gastrointestinal tract. | 2001 Mar |
|
| Hormonal regulation of chicken intestinal NHE and SGLT-1 activities. | 2001 Mar |
|
| Impaired PI 3-kinase activation in adipocytes from early growth-restricted male rats. | 2001 Mar |
|
| Effects of cellular ATP depletion on glucose transport and insulin signaling in 3T3-L1 adipocytes. | 2001 Mar |
|
| Glucose metabolism in perfused mouse hearts overexpressing human GLUT-4 glucose transporter. | 2001 Mar |
|
| Ceramide dissociates 3'-phosphoinositide production from pleckstrin homology domain translocation. | 2001 Mar 1 |
|
| GLUT4 vesicle trafficking in rat adipocytes after ethanol feeding: regulation by heterotrimeric G-proteins. | 2001 Mar 1 |
Patents
Sample Use Guides
no more than 80 to 3000 mg saccharin per kilogram or litre should be used
Route of Administration:
Oral
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:08:05 UTC 2023
by
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on
Fri Dec 15 15:08:05 UTC 2023
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| Record UNII |
I4807BK602
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| Record Status |
Validated (UNII)
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NCI_THESAURUS |
C283
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Food Contact Sustance Notif, (FCN No.) |
FCN NO. 1148
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SACCHARIN SODIUM ANHYDROUS
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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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PRIMARY | RxNorm |
| Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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PARENT -> SALT/SOLVATE | |||
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SOLVATE->ANHYDROUS |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |