@article{ref1,
title="Pharmacological profile of CEB-1957 and atropine toward brain muscarinic receptors and comparative study of their efficacy against sarin poisoning",
journal="Toxicology and applied pharmacology",
year="1998",
author="Trovero, F. and Brochet, D. and Breton, P. and Tambuté, A. and Bégos, A. and Bizot, J. C.",
volume="150",
number="2",
pages="321-327",
abstract="This study consists of two parts, first to compare the pharmacological profile of atropine and CEB-1957 substance toward muscarinic receptor subtypes. In various rat brain structures, binding properties were determined by competition experiments of [3H]pirenzepine, [3H]AF-DX 384, and [3H]4-DAMP in quantitative autoradiography of M1, M2, and M3 muscarinic receptor subtypes, respectively. Competition curves have shown that atropine presents similar nanomolar inhibition constants toward each subtype, while CEB-1957 has distinct affinities (Ki from 0.26 to 73 nM) with the following range order: M3 > or = M2 > M1. The second part is to compare atropine and CEB-1957 (in combination with pralidoxime) for their ability to protect against the lethality induced by 2 x LD50 of the acetylcholinesterase inhibitor sarin. CEB-1957 reduced the mortality at doses 10 times lower than atropine. Finally, from these results, it is proposed that a selective blockade of M2 and M3 receptor subtypes could play a pivotal role in the protective effect against sarin poisoning.<p /><p>Language: en</p>",
language="en",
issn="0041-008X",
doi="10.1006/taap.1998.8423",
url="http://dx.doi.org/10.1006/taap.1998.8423"
}