Nicotinic (a4b2) Receptor Antagonists

Nicotinic α4β2 receptors have high affinity for nicotine and account for >90% of [³H]-nicotine binding to brain tissues. A stoichiometry of (α4)2(β2)3 has been proposed, generating two agonist binding sites consistent with the model of the muscle nAChR.

Manipulation of the stoichiometry of α4β2 nAChRs expressed in Xenopus oocytes indicates that (α4)3(β2)2 nAChRs are also viable, displaying lower affinity for ACh and higher Ca²⁺ permeability; whether ...