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Characterization of the NADPH-dependent metabolism of 17beta-estradiol to multiple metabolites by human liver microsomes and selectively expressed human cytochrome P450 3A4 and 3A5.
TLDR
The NADPH-dependent metabolism of 17beta-estradiol (E2) by liver microsomes from 21 male and 12 female human subjects was characterized and a new monohydroxylated E2 metabolite was found to be one of the major metabolites formed by human livermicrosomes of both genders.
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Separation of Recycling and Reserve Synaptic Vesicles from Cholinergic Nerve Terminals of the Myenteric Plexus of Guinea Pig Ileum
TLDR
As with Torpedo electromotor cholinergic vesicle preparations made under similar conditions the distribution of newly synthesized acetylcholine in the zonal gradient from stimulated preparations was not identical with that of endogenous (d0, [1H]acetate), but corresponded to a subpopulation of denser vesicles that had preferentially taken up newly synthesised transmitter.
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NADPH-dependent metabolism of estrone by human liver microsomes.
TLDR
The NADPH-dependent metabolism of estrone (E1) by liver microsomes of 21 male and 12 female human subjects was characterized and an unidentified monohydroxylated E1 metabolite was found to be one of the major metabolites formed by human liver microSomes of both genders.
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Simultaneous quantitation of arecoline, acetylcholine, and choline in tissue using gas chromatography/electron impact mass spectrometry.
A capillary gas chromatography/mass spectrometry (GC/MS) assay for the simultaneous quantitation of arecoline (ARE), acetylcholine (ACh), and choline (Ch) in biological tissue has been developed. The…
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Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
TLDR
Compounds in which the substituents on the dinitro-N-aryl moiety were relatively small were the best at inhibiting acetylcholinesterase in vitro and were superior to the bis[[(dimethylamino)methyl]furans] in elevating brain ACh levels in mice, probably due to enhanced distribution into the CNS.
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A Comparison of the Cholinergic Activity of Selected H2-Antagonists and Sulfoxide Metabolites
TLDR
Results do not correlate with the in vitro data, where ORF-17578 and ranitidine were the most potent entities with respect to acetylcholinesterase inhibition, followed by nizatidine > cimetidine > famotidine.
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Choline post-mortem increase: effect of tissue, agitation, pH and temperature.
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Comparison of quantitation methods for L-1210 cell populations and evaluation of selected cytotoxic agents in leukemic mice.
TLDR
A more rapid cell-counting technique using an electronic cell counter was developed as an improvement over the slower hemocytometer method, and the decanoate ester was the least toxic compound and was most effective in lengthening the lifespan of the mice.
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Use of radio gas chromatography for monitoring the in vivo labelling of postmortem [3H]choline production.
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Prevention of physostigmine‐, DFP‐, and diazinon‐induced acute toxicity by monoethylcholine and N‐aminodeanol
TLDR
It is proposed that the analogues prevent acetylcholinesterase inhibitor toxicity peripherally by interacting with acetyl Choline, and/or by competing withacetylcholine for binding to cholinoceptors.
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