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The pharmacological action of MT-7.

机译：MT-7的药理作用。

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摘要

The mamba toxin MT-7 is the most selective ligand currently available for the muscarinic M1 receptor subtype. The toxin binds stably to the receptor and blocks the agonist-induced activation non-competitively. Although its mode of action on M1 receptors is not yet fully understood, some of the toxin properties support an allosteric mechanism. Thus, the toxin fails to elicit a complete inhibition of the binding of either the muscarinic antagonist [3H]N-methyl-scopolamine ([3H]NMS) or the agonist [3H]acetylcholine ([3H]ACh). When added to ligand-occupied M1 receptors, the toxin slows the dissociation rate of [3H]NMS and increases that of [3H]ACh. Site-directed mutagenesis studies have provided important information about the toxin amino acid residues which are critical for the stable binding to the receptor and for the allosteric modulation of antagonist dissociation. In vivo studies have shown that the intracerebral injection of MT-7 causes a long-lasting blockade of M1 receptor, thus providing a tool for the characterization of the functional role of this receptor subtype in discrete brain areas.
机译：曼巴毒素MT-7是毒蕈碱M1受体亚型目前可获得的最具选择性的配体。毒素与受体稳定结合，并非竞争性地阻断激动剂诱导的激活。尽管尚未完全了解其对M1受体的作用方式，但某些毒素特性支持变构机制。因此，该毒素不能完全抑制毒蕈碱拮抗剂[3H] N-甲基东sco碱（[3H] NMS）或激动剂[3H]乙酰胆碱（[3H] ACh）的结合。当添加到被配体占据的M1受体中时，该毒素会减慢[3H] NMS的解离速率，并增加[3H] ACh的解离速率。定点诱变研究已经提供了有关毒素氨基酸残基的重要信息，这些残基对于与受体的稳定结合以及拮抗剂解离的变构调节至关重要。体内研究表明，脑内注射MT-7会导致M1受体的长期阻断，从而为表征该受体亚型在离散脑区中的功能作用提供了一种工具。

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