Recent Advances in the Discovery of Nicotinic Acetylcholine Receptor Allosteric Modulators

Author:

Manetti Dina1ORCID,Dei Silvia1ORCID,Arias Hugo R.2,Braconi Laura1ORCID,Gabellini Alessio1ORCID,Teodori Elisabetta1ORCID,Romanelli Maria Novella1ORCID

Affiliation:

1. NEUROFARBA Department, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, 50019 Florence, Italy

2. Department of Pharmacology and Physiology, College of Osteopathic Medicine, Oklahoma State University, Tahlequah, OK 74464, USA

Abstract

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.

Funder

University of Florence Fondo Ricerca Ateneo

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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