Ligand-gated calcium channels

L-type calcium channels (voltage-gated calcium channels L-subtype) Similarity to Diltiazem and a second ligand. ZINC db ( 50 K commercially available subset screened but most filtered to achieve desired PK profile using VolSurf). SHOP similarity, and feature-presence filtering down to 36 compounds 7 hits 18 tested, active in a vasorelaxant assay and some had novel structures. [67]... 

Ca2+ can enter cells via voltage- or ligand-dependent channels and by capacitative entry. These three fundamental mechanisms of regulated calcium ion entry across the plasma membrane involve, respectively, voltage-dependent Ca2+ channels, ligand-gated Ca2+ channels and capacitative Ca2+ entry associated with phospholipase C-coupled receptors. 

Besides sodium channels, other ion channels such calcium- and potassium channels as well as certain ligand-gated channels are affected by local anaesthetics. However, this plays only a minor role for nerve block but may have more impact on adverse effects induced by systemical concentrations of these drags. 

In addition to the pre-synaptic effects, CX3CL1 modulates the functional properties of ligand-gated channels at post-synaptic sites. In SK-N-SH cells, a human neuroblastoma cell line, CX3CL1 reduces the amplitude of NMDA-induced calcium transients (Deiva et al. 2004). In these cells, CX3CL1 application causes a PTX insensitive transient increase in the intracellular Ca " concentration dependent on... 

Figure 2.5. The synapse. GPCR = guanine nucleotide-binding protein-coupled receptor, LGICR = ligand-gated ion channel receptor, SB = synaptic bouton, T = neurotransmitter, YOC = voltage-operated ion channel protein, YOCC = voltage-operated calcium channel protein, Ast = astrocyte, AA = axoaxonal synapse, ASD = axosomatic or axodendritic synapse. GPCR 1 = receptor protein, 2 = G-protein, 3 = enzyme, 4 = ion channel protein.

High-affinity ligand to the a2S-1 subunit of voltage-gated calcium channel... 

Entry through voltage- or ligand-gated calcium channels in the cell membrane. 

Rampe, D. Triggle, D. J. New Synthetic Ligands forL-Type Voltage-Gated Calcium Channels, Prog. Drug Res. 1993, 40, 191. 

FIGURE 10—25. Shown here is normal excitatory neurotransmission at the N-methyW-aspartate (NMDA) type of glutamate receptor. The NMDA receptor is a ligand-gated ion channel. This rapidly transmitting ion channel is an excitatory calcium channel. Occupancy of NMDA glutamate receptors by glutamate causes calcium channels to open and the neuron to be excited for neurotransmission. 

Zhorov BS, Tikhonov DB. Potassium, sodium, calcium and glutamate-gated channels pore architecture and ligand action. J Neurochem. 2004 88 782-799. 

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