AChRβ Activators

Compounds classified as AChRβ Activators have the capacity to directly engage with the nicotinic acetylcholine receptors at various levels of selectivity and efficacy. These activators include both full and partial agonists that can bind to the receptor's orthosteric site where acetylcholine naturally binds, or at allosteric sites, causing a conformational change to the receptor protein and resulting in the opening of the ion channel. This ion channel opening leads to an influx of cations, such as sodium or calcium, which depolarizes the neuron and can initiate a cellular response.

Among these activators, nicotine is one of the most well-known, exerting its effect by mimicking the action of acetylcholine at the receptor, while varenicline and cytisine, with their partial agonist activity, provide a more controlled stimulation of the receptor. The diversity of these compounds provides a range of specificity and efficacy, from the broad-spectrum action of compounds like carbachol to the more targeted action of molecules like PNU-282,987 and 5-Iodo-A-85380, which exhibit a preference for the alpha subunits of the receptor. The molecules Sazetidine-A, PHA-543,613, and ABT-418 display a particular affinity for the alpha4beta2 subtype of the nAChR, which includes the CHRNB1 subunit.