| 词条 | Oltipraz |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 449559107 | IUPAC_name = 4-methyl-5-(2-pyrazinyl)-3-dithiolethione | image = Oltipraz.png | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 64224-21-1 | ATC_prefix = none | ATC_suffix = | PubChem = 47318 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 6N510JUL1Y | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 77319 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 178459 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 43066 | chemical_formula = | C=8 | H=6 | N=2 | S=3 | molecular_weight = 226.34 g/mol | smiles = CC1=C(SSC1=S)C2=NC=CN=C2 | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C8H6N2S3/c1-5-7(12-13-8(5)11)6-4-9-2-3-10-6/h2-4H,1H3 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = CKNAQFVBEHDJQV-UHFFFAOYSA-N }}Oltipraz is an organosulfur compound belonging to the dithiolethione class.[1][2] It acts as a schistosomicide and has been shown in rodent models to inhibit the formation of cancers in the bladder, blood, colon, kidney, liver, lung, pancreas, stomach, and trachea, skin, and mammary tissue.[3][4] Clinical trials of oltipraz have failed to demonstrate efficacy and have shown significant side effects, including neurotoxicity and gastrointestinal toxicity.[3] Oltipraz has also been shown to generate superoxide radical, which can be toxic.[5] References1. ^{{cite journal |vauthors=Prince M, Li Y, Childers A, Itoh K, Yamamoto M, Kleiner HE | title = Comparison of citrus coumarins on carcinogen-detoxifying enzymes in Nrf2 knockout mice | journal = Toxicol. Lett. | volume = 185 | issue = 3 | pages = 180–6 |date=March 2009 | pmid = 19150646 | pmc = 2676710 | doi = 10.1016/j.toxlet.2008.12.014 | url = }} {{antiinfective-drug-stub}}2. ^{{Cite journal|last=Ansari|first=Mohd Imran|last2=Khan|first2=Mohd M.|last3=Saquib|first3=Mohammad|last4=Khatoon|first4=Shahnaaz|last5=Hussain|first5=Mohd Kamil|date=2018-05-01|title=Dithiolethiones: a privileged pharmacophore for anticancer therapy and chemoprevention|journal=Future Medicinal Chemistry|volume=10|issue=10|pages=1241–1260|doi=10.4155/fmc-2017-0281|issn=1756-8927|pmid=29749746}} 3. ^1 {{cite journal |vauthors=Zhang Y, Gordon GB | title = A strategy for cancer prevention: stimulation of the Nrf2-ARE signaling pathway | journal = Mol. Cancer Ther. | volume = 3 | issue = 7 | pages = 885–93 |date=July 2004 | pmid = 15252150 | doi = | url = }} 4. ^{{cite journal |vauthors=Iida K, Itoh K, Kumagai Y, etal |title=Nrf2 is essential for the chemopreventive efficacy of oltipraz against urinary bladder carcinogenesis |journal=Cancer Res. |volume=64 |issue=18 |pages=6424–31 |date=September 2004 |pmid=15374950 |doi=10.1158/0008-5472.CAN-04-1906 |url=http://cancerres.aacrjournals.org/cgi/pmidlookup?view=long&pmid=15374950}} 5. ^{{cite journal |vauthors=Velayutham M, Villamena FA, Fishbein JC, Zweier JL | title = Cancer chemopreventive oltipraz generates superoxide anion radical | journal = Arch. Biochem. Biophys. | volume = 435 | issue = 1 | pages = 83–8 |date=March 2005 | pmid = 15680910 | doi = 10.1016/j.abb.2004.11.028 | url = }} 4 : Antiparasitic agents|Pyrazines|Dithioles|Thiocarbonyl compounds |
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