The effect of mebudipine and dibudipine, two new Ca2+ channel blockers, in comparison with nifedipine on Ca2+ spikes of F1 neuronal soma membrane in Helix aspersa.
Mebudipine and dibudipine are two new dihydropyridine (DHP) Ca2+ channel blockers that have been synthesized by Mahmoudian et al. (1997). In previous studies, they showed considerable relaxant effect on vascular and ileal smooth muscles. These two compounds also reduced the contraction force of rat left atrium (20, 22). In the present study, we attempted to compare the inhibitory actions of these new DHPs and nifedipine on the high threshold Ca2+ spikes of F1 neuronal soma membrane in the subesophageal ganglia of Helix aspersa, using current-clamp method. At a concentration of 1 microM, two new DHP compounds (mebudipine and dibudipine) were tested for their L-type Ca2+ channel blocker activity. Both compounds reversibly reduced the peak amplitude of action potential and after hyperpolarization potential and markedly decreased the duration of Ca2+ spikes. The most potent of these DHPs was mebudipine. Neither the two new DHPs nor nifedipine changed the resting membrane potential in a statistically significant way.
Department of Pharmacology and Toxicology, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, Tehran, Iran.
M
M
Faizi
M
M
Janahmadi
M
M
Mahmoudian
D015761:4-Aminopyridine / Q000494:pharmacology; D000704:Analysis of Variance; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020746:Calcium Channels, L-Type / Q000502:physiology; D020013:Calcium Signaling / Q000187:drug effects* / Q000502:physiology; D004305:Dose-Response Relationship, Drug; D004594:Electrophysiology; D004947:Esophagus / Q000294:innervation; D006372:Helix, Snails; D008564:Membrane Potentials / Q000502:physiology; D009474:Neurons / Q000187:drug effects* / Q000502:physiology; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000494:pharmacology; D018408:Patch-Clamp Techniques
D002121:Calcium Channel Blockers; D020746:Calcium Channels, L-Type; C110813:dibudipine; C110812:mebudipine; D015761:4-Aminopyridine; D009543:Nifedipine; D002118:Calcium