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Bajgar, J. (author), Ševelová, L. (author), Krejčová, G. (author), Fusek, J. (author), Vachek, J. (author), Kassa, J. (author), Herink, J. (author), de Jong, L.P.A. (author), Benschop, H.P. (author)Soman belongs to the most dangerous nerve agents because of the low effectiveness of the presently available antidotes. Soman acts by inhibiting acetylcholinesterase (AChE) both peripherally and centrally, with a subsequent accumulation of neuromediator acetylcholine and other metabolic changes. From the data published in literature it can be...article 2004
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TNO Prins Maurits Laboratorium (author), Langenberg, J.P. (author), de Jong, L.P.A. (author), Benschop, H.P. (author)Several p-nitrophenyl phosphoramidates with the general formula RO(NH2)P(O)OC6H4-p-NO2, in which R = CH2CH3, CH2CH2F, CH2CHF2, CH2CF3, CH2CH2CH2CH3, and CH2CH2Cl, as well as (NH2)2P(O)OC6H4-p-NO2 were administered intravenously to guinea pigs as pretreatment compounds for protection against the lethal effects of 1,2,2-trimethylpropyl...article 1996
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van Helden, H.P.M. (author), de Lange, J. (author), Busker, R.W. (author), Melchers, B.P.C. (author), Medisch Biologisch Laboratorium TNO (author)Isolated rat diaphragm preparations treated with soman or with the irreversible and oxime resistant cholinesterase (ChE) inhibitor S27 (see Compounds) showed a considerable recovery of neuromuscular transmission (NMT) during incubation with the (bis)pyridinium oximes HI-6, HGG-12, P2S and obidoxime. In the soman-treated preparations this NMT...article 1991
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Prins Maurits Laboratorium TNO (author), Ligtenstein, D.A. (author), Moes, G.W.H. (author), Kossen, S.P. (author)In order to visualize the distribution of HI-6 in the rat after iv administration, autoradiographic experiments were carried out with [14C]HI-6, labeled at the carbon of the carboxamide moiety. Autoradiography clearly confirms penetration of HI-6 into the central nervous system. Considerable radioactivity was found in the cerebrum, the...article 1988
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Wolthuis, O. (author), Vanwersch, R.A.P. (author), van der Wiel, H.J. (author), Medisch Biologisch Laboratorium TNO (author)Previous results had shown that bis-pyridinium oximes, particularly HI-6 are quite effective therapeutically in soman-poisoned rats and mice in vivo and in the rat diaphragm preparation in vitro. The aim of the present study was to investigate the efficacy of bis-pyridinium oximes on soman-inhibited neuromuscular transmission in muscle...article 1981
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Benschop, H.P. (author), van den Berg, G.R. (author), van Hooidonk, C. (author), de Jong, L.P.A. (author), Kientz, C.E. (author), Berends, F. (author), Kepner, L.A. (author), Meeter, E. (author), Visser, R.P.L.S. (author), Medisch Biologisch Laboratorium TNO (author)Three new nonquaternary oximes have been evaluated with respect to their antidotal activities against organophosphate poisoning. The oximes 1,2,3-thiadiazole-5-carboxaldoxime (1, pKa = 7.6), 2-methyl-1,3,4-thiadiazole-5-carboxaldoxime (2, pKa = 8.4), and 3-methyl-1,2,4-thiadiazole-5-carboxaldoxime (3, pKa = 7.0) were prepared in yields of 56, 24...article 1979
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Wolthuis, O.L. (author), Clason-van der Wiel, H.J. (author), Visser, R.P.L.S. (author), Medisch Biologisch Laboratorium TNO Chemisch Laboratorium TNO (author)Atropinised anaesthetised rats were injected i.v. with 4, 6 or 8 x LD50 of the organophosphorous anticholinesterase soman. Subsequent treatment with one dose of HS 6 (100 mg/kg, i.v.) delayed respiratory failure by 1 h or more; a further postponement was obtained when an additional HS 6 infusion was given. At the same infusion rate, HS 6 blood...article 1976