M1受体正变构调节剂的发现方法。
M1 receptor positive allosteric modulators discovery approaches.
作者信息
Mandai Takao, Simen Arthur A, Laurenza Antonio, Kimura Haruhide
机构信息
Neuroscience Drug Discovery Unit, Research, Takeda Pharmaceutical Company Limited, Fujisawa, Kanagawa, Japan.
Neuroscience Therapeutic Area Unit, Takeda Development Center Americas, Inc., Cambridge, MA, USA.
出版信息
Trends Pharmacol Sci. 2025 Apr;46(4):298-302. doi: 10.1016/j.tips.2025.03.001. Epub 2025 Mar 25.
The development of M1 muscarinic acetylcholine-receptor-positive allosteric modulators has been hindered by their limited cognitive efficacy and cholinergic side effects. We discuss two unique approaches - low intrinsic agonism and low binding cooperativity - that were developed to address these issues and their therapeutic implications.
M1毒蕈碱型乙酰胆碱受体阳性变构调节剂的研发因认知功效有限和胆碱能副作用而受阻。我们讨论了为解决这些问题及其治疗意义而开发的两种独特方法——低内在激动性和低结合协同性。
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