Mechanism of action of alpha2delta ligands: voltage sensitive calcium channel (VSCC) modulators.
Voltage sensitive calcium channels (VSCCs) have unique structures and functions that distinguish them from other ion channels, especially the voltage sensitive sodium channels (VSSCs). Modulation of VSCCs by certain drugs such as pregabalin and gabapentin via binding to the alpha2delta subunits of VSCCs can lead to anticonvulsant, anxiolytic, and chronic pain-relieving actions.
Neuroscience Education Institute in Carlsbad, Calif., and the Department of Psychiatry at the University of California San Diego, 92009, USA.
Stephen M
SM
Stahl
D000085:Acetates / Q000494:pharmacology*; D000588:Amines; D000700:Analgesics / Q000494:pharmacology; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D015220:Calcium Channels / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D003509:Cyclohexanecarboxylic Acids; D000077206:Gabapentin; D006801:Humans; D008024:Ligands; D008959:Models, Neurological; D000069583:Pregabalin; D020836:Protein Structure, Quaternary / Q000502:physiology; D015222:Sodium Channels / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*
D000085:Acetates; D000588:Amines; D000700:Analgesics; D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D002121:Calcium Channel Blockers; D015220:Calcium Channels; D003509:Cyclohexanecarboxylic Acids; D008024:Ligands; D015222:Sodium Channels; D000069583:Pregabalin; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin