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- W2004751468 abstract "Studies involving the interactions of the crystalline neurotoxin holothurin A with the rat phrenic nerve-diaphragm preparation have shown that an irreversible destruction of the indirectly elicited twitch response can be largely negated by preincubation of the preparation with tiny concentrations of the representative anticholinesterases physostigmine, neostigmine, or galanthamine. This protective action is afforded by concentrations of the anti-acetylcholinesterase agents distinctly below those required to elicit blockade of the tissue-localized esterase, but still in a potency sequence that is roughly proportional to their antfcholinesterasic strengths in vitro. Further, the protection phenomenon itself is readily overridden by concentration increments of a given anti-acetylcholinesterase agent beyond its characteristic optimum value in the tissue bath, up to the point of complete disappearance of the effect. Further experiments with purified subfractions of the total holothurin mixture have pointed to some stringent structural requirements of synaptic receptors susceptible to holothurin attack. Although a chromatographically pure component of the original mixture possesses essentially the same specific activity at the loci controlling nerve-stim- ulated twitch events as the mixture itself, and the loss of two sugar residues at carbon-3 affects the activity picture only moderately, the loss of the half-esterified sulfate function results in an abrupt decrease in blocking potency to virtually the zero level. These results are interpreted in terms of possible mechanisms for interaction of holothurin moieties, degradation products, and competing agents at neuromuscular receptor loci." @default.
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- W2004751468 date "1965-08-01" @default.
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- W2004751468 title "Some structural requirements underlying holothurin a interactions with synaptic chemoreceptors" @default.
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- W2004751468 doi "https://doi.org/10.1016/0006-2952(65)90301-1" @default.
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