AChRβ3 Inhibitors

AChRβ3 inhibitors are chemical agents that can prevent or diminish the activation of nicotinic acetylcholine receptors containing the β3 subunit. These compounds exhibit diverse structures and pharmacological profiles, ranging from non-competitive antagonists, like mecamylamine, which block the ion channel of the receptor, to competitive antagonists, such as hexamethonium and trimethaphan, which compete with acetylcholine for binding sites. The inhibitors can affect the receptor by either preventing the ion channel from opening, which is essential for the propagation of neural signals, or by stabilizing the receptor in its inactive form.

The compounds listed function primarily by interrupting the normal signaling cascade initiated by the binding of acetylcholine to nAChRs. For instance, mecamylamine and bupropion are known to cross the blood-brain barrier and inhibit central nAChRs, which can include those with the β3 subunit. Ganglionic blockers like hexamethonium and chlorisondamine work by competitively inhibiting nAChRs at autonomic ganglia, which can influence peripheral nAChRs containing the β3 subunit. Other compounds, such as α-conotoxin and α-bungarotoxin, are found in animal venoms and have evolved to target nAChRs with high specificity and potency, possibly affecting nAChRs that contain the β3 subunit. Although these inhibitors are not selective for the β3 subunit, they provide valuable insights into the functional modulation of nAChRs and their pharmacological intervention. The chemicals listed are known to inhibit nicotinic acetylcholine receptors (nAChRs) in general or are broad-spectrum nAChR antagonists, and they can affect various subtypes of nAChRs, potentially including those that incorporate the AChRβ3 subunit.