Modulation of K(+)-induced synaptosomal calcium influx by gabapentin.
Gabapentin, a drug useful in several neurological and psychiatric disorders, decreased K(+) (15 mM)-induced [Ca(2+)](i) increase in Fura-PE3-loaded rat neocortical synaptosomes (IC(50)=9.7 microM; submaximal inhibition of 28.6%). This effect may indicate a selective modulation of presynaptic Ca(2+) influx in response to depolarizing (pathological) conditions causing excessive neurotransmitter release.
Meder
W P
WP
Pfizer Global Research & Development, Department of Neuroscience Therapeutics, Ann Arbor, MI 48105, USA. wolfgang.meder@wl.com
Dooley
D J
DJ
D000085:Acetates / Q000494:pharmacology*; D000588:Amines; D000818:Animals; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000494:pharmacology*; D003509:Cyclohexanecarboxylic Acids; D004305:Dose-Response Relationship, Drug; D000077206:Gabapentin; D008297:Male; D009994:Osmolar Concentration; D011188:Potassium / Q000008:administration & dosage / Q000494:pharmacology / Q000502:physiology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013574:Synaptosomes / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid
D000085:Acetates; D000588:Amines; D002121:Calcium Channel Blockers; D003509:Cyclohexanecarboxylic Acids; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin; D011188:Potassium; D002118:Calcium