Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators

被引：18

作者：

Manetti, Dina ^{[1
]}

Dei, Silvia ^{[1
]}

Arias, Hugo R. ^{[2
]}

Braconi, Laura ^{[1
]}

Gabellini, Alessio ^{[1
]}

Teodori, Elisabetta ^{[1
]}

Romanelli, Maria Novella ^{[1
]}

机构：

[1] Univ Florence, NEUROFARBA Dept, Sect Pharmaceut & Nutraceut Sci, I-50019 Florence, Italy

[2] Oklahoma State Univ, Coll Osteopath Med, Dept Pharmacol & Physiol, Tahlequah, OK 74464 USA

来源：

MOLECULES | 2023年 / 28卷 / 03期

关键词：

positive allosteric modulator; negative allosteric modulator; desensitization; alpha; 7; 4; beta; 2; nicotinic acetylcholine receptor; BINDING-SITES; PHARMACOLOGICAL CHARACTERIZATION; ALTERNATE STOICHIOMETRIES; MECAMYLAMINE ENANTIOMERS; SUBUNIT INTERFACES; IN-VITRO; ALPHA-7; ALPHA-4-BETA-2; ACTIVATION; POTENTIATION;

D O I：

10.3390/molecules28031270

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 alpha 7 and alpha 4 beta 2. 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.

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页数：24

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