Cys-loop receptors

Key Words Serotonin3 receptor 5-hydroxytryptamine3 receptor Cys-loop receptor ligand-gated ion channel ionotropic receptor neurotransmitter binding site. 

The insect GABA receptor-chloride ionophore complex is found in the CNS and also at peripheral neuromuscular sites. GABA receptors belong to a superfamily of ligand-gated ion channels known as Cys-loop receptors that include nicotinic acetylcholine receptors and glutamate-gated chloride channels (Lester, 2004). Cys-loop receptors are so named because... 

Although Dendrobium species are much better known as ornamental plants and for their use in traditional medicine, their alkaloids, the dendrobines, are also convulsants (2). The effects of dendrobinium chloride intoxication resemble more those of strychnine intoxication than those of picrotoxinin intoxication (240). The minimal lethal dose (intravenous) in rats and mice is 20 mg/kg. The toxicity of the picrotoxanes is attributable to their ability to overcome the blood-brain barrier and to bind to inhibitory Cys-loop receptors of the postS3napses of the CNS. 

Sine SM, Engel AG (2006) Recent Advances in Cys-loop Receptor Structure and Function. 

Allosteric modulation of ligand-gated ion channek [137], such as the Cys-loop receptors [138], and state-dependent modulation have yet to be imderstood more deeply in order to assist library design. 

Chang, Y Huang, Y., and Whiteaker, P. (2010) Mechanism of allosteric modulation of the cys-loop receptors. Pharmaceuticals, 3, 2592-2609. 

D. D. Mowrey, M. N. Kinde, Y. Xu and P. Tang, Atomistic Insights into Human Cys-Loop Receptors by Solution NMR, Biochim. Biophys. Acta, Bio-memhr., 2015, 1848, 307. 

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