Inhibitory effect of 0,0-bisacetyldaurisoline on Ca2+ influx into synaptosomes.
The inhibitory effects of 0,0-bisacetyldaurisoline (BDSL) on 45Ca2+ uptake and [3H]GABA release from synaptosomes were investigated. BDSL (1-100 mumol.L-1) produced a concentration-related inhibition of high K(+)-stimulated 45Ca2+ uptake and [3H]GABA release (IC50 = 5.6 +/- 0.7 and 31.4 +/- 2.3 mumol.L-1, respectively) in synaptosomes but verapamil (Ver) was only weakly active. Neither BDSL (100 mumol.L-1) nor Ver (100 mumol.L-1) modified 45Ca2+ uptake in control medium (K+ 5 mmol.L-1 resting uptake) and [3H]GABA release in Ca(2+)-free medium (K+ 45 mmol.L-1 basal release). The results suggest that BDSL may be a potent Ca2+ channel blocker in neurons.
Lu
Y M
YM
Department of Molecular Pharmacology, Naval Neurobiology Research Centre, Nanjing, China.
Liu
G Q
GQ
D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D044182:Benzylisoquinolines; D001693:Biological Transport, Active / Q000187:drug effects; D002118:Calcium / Q000493:pharmacokinetics*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D013574:Synaptosomes / Q000378:metabolism*; D014700:Verapamil / Q000494:pharmacology; D005680:gamma-Aminobutyric Acid / Q000378:metabolism
D000470:Alkaloids; D044182:Benzylisoquinolines; D002121:Calcium Channel Blockers; C076420:O,O-bisacetyldaurisoline; D005680:gamma-Aminobutyric Acid; D014700:Verapamil; D002118:Calcium