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Archives of Toxicology, 2002
The well-documented efficacy of HI 6 dichloride in reactivating acetylcholinesterase (AChE) inhibited by nerve agents is curtailed by its poor water-solubility at temperatures below 10 degrees C. This drawback can be circumvented by using HI 6 dimethanesulfonate, which has been developed in our laboratory.
S, Krummer +3 more
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The well-documented efficacy of HI 6 dichloride in reactivating acetylcholinesterase (AChE) inhibited by nerve agents is curtailed by its poor water-solubility at temperatures below 10 degrees C. This drawback can be circumvented by using HI 6 dimethanesulfonate, which has been developed in our laboratory.
S, Krummer +3 more
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Drug Development and Industrial Pharmacy, 1995
AbstractA stability-indicating reversed-phase high performance liquid chromatographic method was developed for the detection of HI-6 and its degradation products under accelerated degradation conditions. The degradation kinetics of HI-6 in aqueous solution over a pH range of 1.14 to 5.54 and its stability in propylene glycol or polyethylene glycol 400 ...
Da-Peng Wang, Jeng-Dong Lee, Rong-An Lin
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AbstractA stability-indicating reversed-phase high performance liquid chromatographic method was developed for the detection of HI-6 and its degradation products under accelerated degradation conditions. The degradation kinetics of HI-6 in aqueous solution over a pH range of 1.14 to 5.54 and its stability in propylene glycol or polyethylene glycol 400 ...
Da-Peng Wang, Jeng-Dong Lee, Rong-An Lin
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The pharmacokinetics of HI‐6 in beagle dogs
Biopharmaceutics & Drug Disposition, 1983AbstractThe pharmacokinetics of HI‐6 were studied following intravenous administration to beagle dogs (n = 7). The bioavailability of two different strength intramuscularly administered doses was also determined in the same animals. After a 20 mg kg−1 intravenous dose, the mean (±S.D.) initial HI‐6 plasma concentration was 93·1 ± 10·μg ml−1.
K J, Simons, C J, Briggs
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Pharmacology of HI-6, an H-series oxime
Canadian Journal of Physiology and Pharmacology, 1989HI-6 is an oxime experimentally developed for reactivation of previously untreatable soman-phosphorylated acetylcholinesterase. It has been shown to be effective in restoring acetylcholinesterase activity after poisoning with other "nerve agents" namely VX and sarin; however, its antidotal qualities for the treatment of organophosphorus pesticide ...
C G, Rousseaux, A K, Dua
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International Journal of Pharmaceutics, 1996
To oppose the rapid onset of cholinergic crisis after poisoning with highly toxic organophosphorus compounds, atropine in combination with a cholinesterase reactivator should be administered as early as possible. Due to its broader antidotal spectrum against nerve agents, the second-generation oxime HI 6 appears suitable to replace the marketed oximes,
Horst Thiermann +2 more
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To oppose the rapid onset of cholinergic crisis after poisoning with highly toxic organophosphorus compounds, atropine in combination with a cholinesterase reactivator should be administered as early as possible. Due to its broader antidotal spectrum against nerve agents, the second-generation oxime HI 6 appears suitable to replace the marketed oximes,
Horst Thiermann +2 more
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Non-reactivating effects of HI-6 on hippocampal neurotransmission
Archives of Toxicology, 1994Effects of the oxime HI-6, unrelated to reactivation of acetylcholinesterase (AChE), on field potentials in the dentate gyrus of the rat hippocampus following AChE inhibition, were investigated both in vitro and in vivo. In hippocampal slices, AChE inhibition decreased the perforant path evoked population spike amplitude (PSA).
Melchers, B.P.C. +4 more
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Cardiopulmonary effects of HI-6 treatment in soman intoxication
Journal of Applied Toxicology, 2001The cardiopulmonary effects of HI-6, together with atropine and soman, were studied in the rat. HI-6 is an effective antidote in acute poisoning with the nerve agent soman. The therapeutic efficiency of HI-6 is still unclear and cannot be explained entirely by the HI-6 reactivating ability of acetylcholinesterase (AChE).
A, Göransson-Nyberg, G, Cassel
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DFT conformational studies of the HI‐6 molecule
International Journal of Quantum Chemistry, 2005AbstractA systematic study of the oxime HI‐6 [1‐(2‐hydroxyiminomethyl‐1‐pyridinium)‐1‐(4‐carboxy‐aminopyridinium)dimethyl ether] hydrochloride, which is one of the most promising antidotes against soman intoxication, was carried out using density functional theory with the B3LYP (Becke, Lee, Yang, and Parr) method and the 6‐31+G*, 6‐31+G*, and 6‐31+G**
Gustavo R. Silva +2 more
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Bioavailability and disposition kinetics of HI‐6 in Beagle dogs
Biopharmaceutics & Drug Disposition, 1993AbstractThe absorption and disposition kinetics of HI‐6 were determined in Beagle dogs given single doses (25 mg kg−1) of the drug by the intravenous, intramuscular, and oral routes. Concentrations of the oxime in plasma and urine were measured by HPLC.
J D, Baggot +4 more
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Photostability of antidotal oxime HI‐6, impact on drug development
Drug Testing and Analysis, 2012HI‐6 exhibits superior efficacy in the therapy of intoxication by different highly toxic organophosphorus nerve agents. Therefore HI‐6 is a promising candidate for the development of new antidotes against nerve agents. For ethical and safety reasons antidotes containing HI‐6 should get marketing authorization.
Reinhard, Bogan +3 more
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