Effects of clomipramine on neuronal nicotinic acetylcholine receptors

Tricyclic antidepressants inhibit homomeric Cys-loop receptors by acting at different conformational states

“…These results show that doxepin act on α7-5HT 3A (HC) in a manner consistent with a noncompetitive mechanism. This observation is in great agreement with previous studies of the actions of different types of antidepressants on Torpedo, muscle and neuronal nicotinic receptors (Eldefrawi et al, 1981;Schofield et al, 1981;García-Colunga et al, 1997;García-Colunga and Miledi, 1999;López-Valdez et al, 2002;Gumilar et al, 2003).…”

Different Classes of Antidepressants Inhibit the Rat α7 Nicotinic Acetylcholine Receptor by Interacting within the Ion Channel: A Functional and Structural Study

“…These findings are also consistent with values of the electric distance (fraction of the electrical field sensed by the compound at its binding site in the ion channel), which ranged from 0.10 to 0.40 for different antidepressants [12,13,16,43]. It is interesting to note that, in addition to antidepressants, other substances interact within the ion channel of nAChRs in similar regions, including tetracaine, carbamazepine, barbiturates, and anesthetics, such as phencyclidine and ketamine [12][13][14][15]17,29,44].…”

SSRI antidepressants do not confound single photon emission computed tomography (SPECT) imaging studies using the α4β2 nicotinic acetylcholine receptor [123I]5‐I‐A85380 ligand: In vivo and in vitro evidence

“…Monoamine-uptake inhibitors reduce cholinergic currents and imipramine regulates, reversibly and noncompetitively, neuronal a4b2 and muscle AChRs through similar mechanisms (López-Valdés and García-Colunga, 2001). More recently this theory was confirmed by the same group (López-Valdés et al, 2002), finding that clomipramine reversibly and noncompetitively regulates neuronal a4b2 nicotinic acetylcholine receptors by blocking the open receptor-channel complex at a site close to the extracellular vestibule of the channel.…”