[(3)H]chlorpromazine photolabeling of the torpedo nicotinic acetylcholine receptor identifies two state-dependent binding sites in the ion channel.

@article{Chiara20093HchlorpromazinePO,
  title={[(3)H]chlorpromazine photolabeling of the torpedo nicotinic acetylcholine receptor identifies two state-dependent binding sites in the ion channel.},
  author={David C. Chiara and Ayman K Hamouda and Michael R. Ziebell and Luis A Mejia and Galo Garcia and Jonathan B. Cohen},
  journal={Biochemistry},
  year={2009},
  volume={48 42},
  pages={10066-77}
}
Chlorpromazine (CPZ), a potent nicotinic acetylcholine receptor (nAChR) noncompetitive antagonist, binds with higher affinity in the ion channel in the desensitized state than in the closed channel state and with low affinity to additional sites in nAChR-rich membranes. For nAChR equilibrated with agonist, we confirm previous reports that [(3)H]CPZ occupies a site near the cytoplasmic end of the M2 ion channel domain, photolabeling positions M2-2, M2-6, and/or M2-9 in each subunit. We find that… CONTINUE READING