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Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators.
Molecules ( IF 4.2 ) Pub Date : 2023-01-28 , DOI: 10.3390/molecules28031270
Dina Manetti 1 , Silvia Dei 1 , Hugo R Arias 2 , Laura Braconi 1 , Alessio Gabellini 1 , Elisabetta Teodori 1 , Maria Novella Romanelli 1
Molecules ( IF 4.2 ) Pub Date : 2023-01-28 , DOI: 10.3390/molecules28031270
Dina Manetti 1 , Silvia Dei 1 , Hugo R Arias 2 , Laura Braconi 1 , Alessio Gabellini 1 , Elisabetta Teodori 1 , Maria Novella Romanelli 1
Affiliation
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent agonists, allosteric activating PAMs and neutral or silent allosteric modulators are compounds capable of modulating the nicotinic receptor by interacting at allosteric modulatory sites distinct from the orthosteric sites. This survey is focused on the compounds that have been shown or have been designed to interact with nicotinic receptors as allosteric modulators of different subtypes, mainly α7 and α4β2. Minimal chemical changes can cause a different pharmacological profile, which can then lead to the design of selective modulators. Experimental evidence supports the use of allosteric modulators as therapeutic tools for neurological and non-neurological conditions.
中文翻译:
烟碱型乙酰胆碱受体变构调节剂发现的最新进展。
正变构调节剂 (PAM)、负变构调节剂 (NAM)、沉默激动剂、变构激活 PAM 和中性或沉默变构调节剂是能够通过在不同于正构位点的变构调节位点相互作用来调节烟碱受体的化合物。该调查的重点是已显示或已设计为与烟碱受体相互作用的化合物,作为不同亚型的变构调节剂,主要是 α7 和 α4β2。最小的化学变化会导致不同的药理学特征,从而导致选择性调节剂的设计。实验证据支持使用变构调节剂作为神经和非神经疾病的治疗工具。
更新日期:2023-01-28
中文翻译:

烟碱型乙酰胆碱受体变构调节剂发现的最新进展。
正变构调节剂 (PAM)、负变构调节剂 (NAM)、沉默激动剂、变构激活 PAM 和中性或沉默变构调节剂是能够通过在不同于正构位点的变构调节位点相互作用来调节烟碱受体的化合物。该调查的重点是已显示或已设计为与烟碱受体相互作用的化合物,作为不同亚型的变构调节剂,主要是 α7 和 α4β2。最小的化学变化会导致不同的药理学特征,从而导致选择性调节剂的设计。实验证据支持使用变构调节剂作为神经和非神经疾病的治疗工具。