• Aminopterin was discontinued by Lederle Laboratories in favor of methotrexate due to manufacturing difficulties of the former. (wikipedia.org)
  • The use of aminopterin in cancer treatment was supplanted in the 1950s by methotrexate due to the latter's better therapeutic index in a rodent tumor model. (wikipedia.org)
  • Now in a more pure preparation and supported by laboratory evidence of superior tumor cell uptake in vitro, aminopterin is being investigated in clinical trials in leukemia as a potentially superior antifolate to methotrexate. (wikipedia.org)
  • Similar congenital abnormalities have been documented with methotrexate, and collectively their teratogenic effects have become known as the fetal aminopterin syndrome. (wikipedia.org)
  • This is a double-blind, randomized, placebo-controlled, dose ranging study that will evaluate the safety, efficacy, and pharmacokinetic properties (the absorption, distribution and excretion) of aminopterin following oral administration by subjects with active rheumatoid arthritis (≥ 6 tender and ≥ 6 swollen joints) who have not been treated with methotrexate (MTX). (clinicaltrials.gov)
  • A series of novel hydrogen peroxide sensitive prodrugs of methotrexate (MTX) and aminopterin (AMT) were synthesized and evaluated for therapeutic efficacy in mice with collagen induced arthritis (CIA) as a model of chronic rheumatoid arthritis (RA). (worldwidescience.org)
  • Congenital Cardiac Defects: A Possible Association of Aminopterin Syndrome and In Utero Methotrexate Exposure? (biomedsearch.com)
  • We report two patients who presented with classic features of aminopterin syndrome combined with significant congenital cardiac malformations after first-trimester in utero methotrexate exposure. (biomedsearch.com)
  • Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues. (medchemexpress.com)
  • Aminopterin and methotrexate are widely used in selection media (such as HAT medium ) for cell culture . (wikidoc.org)
  • Four folate analogues, methotrexate, aminopterin, 10-deazaaminopterin, and 10-ethyl-10-deazaaminopterin were assessed for their ability to be metabolized to poly-γ-glutamyl derivatives in three tumor lines which vary in their sensitivity to these agents. (aacrjournals.org)
  • Cytotoxicity of the four analogues against the murine L1210 leukemia and the human Manca B cell leukemia, as determined by a 3-h clonogenic assay, showed aminopterin and the two 10-deazaaminopterin compounds to be approximately equivalent for each cell type and were 3- to 10- (L1210) and 7- to 14-fold (Manca) more potent than methotrexate. (aacrjournals.org)
  • In murine Sarcoma 180 cells, 10-ethyl-10-deazaaminopterin and aminopterin were similarly potent but were 5- to 10-fold more potent than 10-deazaaminopterin and 40- to 80-fold more potent than methotrexate. (aacrjournals.org)
  • In L1210 cells incubated for 3 h with drug, efflux of methotrexate and aminopterin polyglutamates was found to be slower than the parent drug and decreased with the addition of polyglutamyl residues. (aacrjournals.org)
  • In contrast, the efflux of methotrexate and aminopterin diglutamates from cells preloaded with these derivatives and the parent compounds was the same, and efflux overall was markedly more rapid. (aacrjournals.org)
  • The New York State Food Laboratory has identified the presence of aminopterin in all of the samples of cat and. (jonbarron.org)
  • Fetal aminopterin syndrome is a condition affecting babies whose mothers were exposed to the chemical aminopterin or methotraxate during pregnancy. (diseaseinfosearch.org)
  • Symptoms of fetal aminopterin syndrome depend on how early in pregnancy the woman is exposed to aminopterin or methotraxate and the dosage of the medication being used. (diseaseinfosearch.org)
  • There is no cure for fetal aminopterin syndrome , though symptoms can be managed. (diseaseinfosearch.org)
  • Following organizations serve the condition "Fetal Aminopterin Syndrome" for support, advocacy or research. (diseaseinfosearch.org)
  • Finding the right clinical trial for Fetal Aminopterin Syndrome can be challenging. (diseaseinfosearch.org)
  • The terms "Fetal Aminopterin Syndrome" returned 0 free, full-text research articles on human participants. (diseaseinfosearch.org)
  • According to ClinicalTrials.gov there are currently 0 additional "open" studies for "Fetal Aminopterin Syndrome" (open studies are recruiting volunteers) and 0 "Fetal Aminopterin Syndrome" studies with "all" status. (diseaseinfosearch.org)
  • 2.Cell fusion to produce hybridomas: Myeloma cells are immortalized cells that are refined with 8 azaguanine to ensure their sensitivity to the hypoxanthine aminopterin-thymidine (HAT) choice medium utilized after cell combination. (maryelizabethbodycare.com)
  • Peripheral blood lymphocytes from "old" male individuals and "young" controls were fused with a Chinese hamster cell line (CHO-YH21), yielding 10 HAT-resistant rodent-human clones from the old propositi and 22 from the young controls (HAT = hypoxanthine/aminopterin/thymidine). (nih.gov)
  • Aminopterin (or 4-aminopteroic acid), the 4-amino derivative of folic acid, is an antineoplastic drug with immunosuppressive properties often used in chemotherapy. (wikipedia.org)
  • In the early 1940s, the first chemotherapy trial in children used a drug called aminopterin , which suppresses the immune system. (theconversation.com)
  • The purpose of this study is to determine whether aminopterin is effective in the treatment of rheumatoid arthritis (RA). (clinicaltrials.gov)
  • The study hypothesis is that the 3 mg LD-aminopterin per week is effective at treating rheumatoid arthritis compared to placebo. (clinicaltrials.gov)
  • Effect of aminopterin in rheumatoid arthritis and psoriasis. (springer.com)
  • When a similar cluster of abnormalies appears in the absence of exposure to antifolates it is referred to as aminopterin-like syndrome without aminopterin. (wikipedia.org)
  • There is now a well-defined syndrome of congenital anomalies associated with the use of aminopterin. (biomedsearch.com)
  • Aminopterin works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase. (wikipedia.org)
  • While working at Harvard Medical School on a research project funded by a grant from the American Cancer Society, he carried out both the preclinical and clinical evaluation of aminopterin (synthesized by Yellapragada Subbarow), a folate antagonist in childhood acute lymphoblastic leukemia. (wikipedia.org)
  • He then helped develop the drug aminopterin that targets folate metabolism. (theconversation.com)
  • The antifolate activity of aminopterin was first used by Sidney Farber in 1947 to induce remissions among children with leukemia . (wikidoc.org)
  • Aminopterin was later marketed by Lederle Laboratories (Pearl River, New York) in the United States from 1953 to 1964 for the indication of pediatric leukemia. (wikipedia.org)
  • The apparently mistaken association of aminopterin with its use as a rodenticide likely dates back to a 1951 patent issued to the American Cyanamid Company (then the holding company of Lederle Laboratories) that is commonly cited by a variety of reference textbooks. (wikipedia.org)
  • [3] [4] Aminopterin je kasnije prodavala kompanija Lederle Laboratories (Pearl River, Njujork ) u SAD od 1953 do 1964 za pedijatrijsku leukemiju . (wikipedia.org)
  • Aminopterin i metotreksat su široko korišćeni u selekciji medija (kao što je HAT medijum ) za ćelijske kulture . (wikipedia.org)
  • Aminopterin se je nekoč uporabljal za zdravljenje raka , dandanes pa ga je povsem nadomestil metotreksat , ki je spojina s podobno strukturo. (wikipedia.org)
  • The first suggestions that folic acid antagonists were teratogenic in humans were based on reports of failed terminations in mothers given aminopterin in the first trimester. (biomedsearch.com)
  • Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a K i of 3.7 pM. (medchemexpress.com)
  • The IC 50 value of Aminopterin (4-Aminofolic acid) against CCRF-CEM cells during 72 h of exposure is 4.4 nM [2] . (medchemexpress.com)
  • Aminopterin (4-Aminofolic acid) produces a marked inhibition of mitosis in low concentrations in human leukemic leukocytes [4] . (medchemexpress.com)
  • His team gave 16 infants and children with acute lymphoblastic leukemia a folic acid inhibitor, aminopterin -10 showed improvement by clinical and hematologic parameters after three months. (wikipedia.org)
  • Aminopterin je sintetički derivat pterina . (wikipedia.org)
  • Aminopterin (4-aminopterojska kislina) je 4- amino derivat folne kisline , ki izkazuje imunosupresivno in citostatično delovanje. (wikipedia.org)
  • Separately, New York state officials, who said they discovered aminopterin -- a substance used in rat poison -- in tainted pet food last week, said they have no doubt that melamine is present in the recalled food. (reuters.com)
  • Since neither aminopterin nor melamine are compounds that should be found in pet food, it is important for full public disclosure," said New York State Department of Agriculture and Markets Commissioner Patrick Hooker. (reuters.com)
  • Acute Renal Failure (ARF) from the ingestion of aminopterin and/or melamine (most likely the latter). (itchmo.com)
  • However, in Sarcoma 180 cells, only aminopterin polyglutamates reached a similar maximum percentage of accumulation, while lower relative polyglutamate levels were achieved with the other analogues. (aacrjournals.org)
  • Accumulation of individual polyglutamates in each cell line was similar for all analogues except aminopterin. (aacrjournals.org)
  • Aminopterin dejstvuje kao inhibitor enzima dihidrofolat reduktaze . (wikipedia.org)
  • Aminopterin , 4-amino analog folne kiseline , je antineoplastični lek sa imunosupresivnim osobinama koji se koristi u hemoterapiji . (wikipedia.org)
  • Aminopterin has a potent effect on leukaemia cells growing in a test tube. (theconversation.com)
  • Aminopterin has a single-dose LDLo of 2.5 mg/kg when orally administered to rats. (wikipedia.org)
  • Edatrexate (10-ethyl-deaza-aminopterin) (NSC #626715) with or without leucovorin rescue for malignant mesothelioma. (duke.edu)
  • The influence of aminopterin on limb regeneration in Ambystoma mexicanum. (medchemexpress.com)
  • The reference to the use of Aminopterin as a rodenticide (i.e. rat poison) dates back to a 1951 patent issued to the American Cyanamid Company that is commonly cited by a variety of reference textbooks including the Merck Manual, although the use of aminopterin as a rodenticide was later disputed. (wikipedia.org)
  • Their findings contradict the New York State Food Laboratory's tests, which pointed to aminopterin - a rat poison - as the likely culprit. (redorbit.com)
  • To address this issue and understand how dosing affects antifolate efficacy in AD, we examined the efficacy and safety of different oral doses and schedules of LD- aminopterin in the canine model of AD. (worldwidescience.org)
  • During the period Aminopterin was marketed, the agent was used off-label to safely treat over 4,000 patients with psoriasis in the United States, producing dramatic clearing of lesions. (wikipedia.org)
  • Aminopterin for psoriasis: A decade's observation. (wikipedia.org)
  • Newborns who survived after aminopterin exposure were noted for years to have defects of the neural tube, skull, or limbs. (biomedsearch.com)
  • Although the use of aminopterin as a rodenticide is widely asserted on the web and elsewhere, there is no evidence that it has ever been used for that purpose either in the United States or elsewhere in the world. (wikidoc.org)
  • The FDA, however, has still not confirmed the presence of aminopterin in the recalled pet food. (reuters.com)
  • On March 23, 2007, ABC News reported that aminopterin was the chemical linked to the 2007 Menu Foods pet food contamination incident. (wikipedia.org)
  • Tests at the University of Guelph in Ontario, Canada detected aminopterin in some pet food samples, but only in concentrations of parts per billion or parts per trillion, amounts too low to cause the symptoms seen. (wikipedia.org)
  • Nor was it clear why earlier tests identified the foreign agent as aminopterin, a finding U.S. Food and Drug Administration officials said they were unable to confirm. (redorbit.com)
  • Using step-wise selection, lines of mouse L-cells were obtained (clones B-82, TK-), resistance to aminopterin (AP) of which exceeds resistance of parental cells by 10 3 -5 x 10 4 times. (worldwidescience.org)
  • Aminopterin was accumulated mainly as the diglutamate, particularly in Manca cells where 70% of total drug was in the diglutamate form within the first 3 h and remained the predominant form for 24 h. (aacrjournals.org)
  • He tested aminopterin in 16 children with leukaemia and obtained temporary remission in ten of them. (theconversation.com)
  • Aminopterin is no longer used, but methotraxate may still be used to treat some conditions such as cancer. (diseaseinfosearch.org)
  • A structurally similar antifolate, aminopterin, also reduced the arthritis. (nih.gov)
  • These same reports stated that the FDA had failed to find evidence of aminopterin in the wheat gluten. (wikipedia.org)
  • Aminopterin is widely used in selection media (such as HAT medium) for cell culture, particularly in the development of hybridomas, which secrete monoclonal antibodies. (wikipedia.org)