A hydrophobic photolabel inhibits nicotinic acetylcholine receptors via open-channel block following a slow step.

@article{Forman1999AHP,
  title={A hydrophobic photolabel inhibits nicotinic acetylcholine receptors via open-channel block following a slow step.},
  author={Stuart A. Forman},
  journal={Biochemistry},
  year={1999},
  volume={38 44},
  pages={14559-64}
}
3-(Trifluoromethyl)-3-(m-iodophenyl)diazirine (TID) is a hydrophobic inhibitor of nicotinic acetylcholine receptors (nAChRs) and a photolabel that incorporates both at the lipid-protein interface and within the gated pore. On the basis of Torpedo vesicle studies, TID is thought to selectively inhibit the closed nAChR state. The nAChR site(s) mediating TID inhibition is unknown. We investigated the state dependence and kinetics of TID inhibition electrophysiologically using rapidly superfused… CONTINUE READING