Molecular Pharmacological Studies on Drug-Receptor Complexes System in Drug Action. I. Antagonism to Acetylcholine of Organophosphorous Compounds.
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The inhibitory action of organophosphates against acetylcholine (ACh), and cholinesterase (ChE) in vitro and in vivo has been observed using parathion, methylparathion, DFP, DDVP, dipterex, metasystox and TEPP. These experiments gave the following results : 1) The investigated organophosphates produced more and less a reversible inhibitory effect against ACh upon the isolated intestinal segments of mice. The stronger anti-ChE agent (e.g. DFP, TEPP) produced a terrible rhythmical motility, but was remarkably less effective inhibiting against ACh than parathion which was found as a comparatively strong anti-ACh agent. 2) The after-effect of DFP and parathion was observed in intestinal muscle and its difference produced by having an affinity for such two different points of action as ChE and ACh receptor was discussed. 3) Anti-ACh activity and anti-ChE activity in vitro (by Warburg method) and in vivo (by the fall effect of blood pressure) of the above organophosphates were measured and compared with each other. The more effective anti-ACh activity was, the less effective anti-ChE activity was. 4) The antiacetylcholine action by some of organophosphates were measured using the rectus abdominis of frog treated with neostigmine, and then were compared with anti-ChE effects and lethal doses (LD 50) to suggest the possibility that the organophosphorus poisoniong in mammals is also produced by blocking ACh, besides inhibiting ChE.
- 1963-01-25
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関連論文
- Molecular Pharmacological Studies on Drug-Receptor Complexes System in Drug Action. I. Antagonism to Acetylcholine of Organophosphorous Compounds.
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