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Effect of CD349, a new dihydropyridine derivative calcium antagonist, on the voltage-dependent calcium currents in isolated mammalian brain neurons

Effect of CD349, a new dihydropyridine derivative calcium antagonist, on the voltage-dependent calcium currents in isolated mammalian brain neurons. Oyama, Y.; Nakaye, T.; Akaike, N.; Tsuchida, K. (Sch. Med., Tohoku Univ.,, Sendai 980, Japan). Arch.Chemical with cas number 88594-08-5 also plays role. Int. Pharmacodyn. Ther., 313, 47-62 (English) 1991. CODEN: AIPTAK. ISSN: 0003-9780. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of CD349 [2-nitratopropyl-3-nitratopropyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydr opyridine-3,5-dicarboxylate], a dihydropyridine deriv. Ca2+ antagonist, were studied on low and high voltage-activated Ca2+ currents in single pyramidal neurons isolated from the rat hippocampal CA1 region. CD349 inhibited the peak amplitude of the low voltage-activated Ca2+ current in a concn.-dependent manner with a threshold concn. of about 10--7 M. The concn. for half-max. inhibition was 1.5 x 10-6 M. At 10-5 M or more, a complete suppression of the low voltage-activated Ca2+ current was obsd. There was no apparent effect on the current-voltage relationship and the current kinetics (rising and decaying phases of the current). The inhibitory potency of CD349 was similar to that of nicardipine. CD349, at a concn. of 10-6 M (near the half-max. inhibition concn.), delayed the reactivation and enhanced voltage- and time-dependently the inactivation of the low voltage-activated Ca2+ channel, suggesting that CD349 preferentially binds to the inactivated Ca2+ channel. CD349 also decreased the peak amplitude of the high voltage-activated Ca2+ current at half-max. inhibition concns. of 5.7 x 10-6 M. The current kinetics of the high voltage-activated Ca2+ current were slightly accelerated without shifting the current-voltage relationship in the presence of 10-5 M of CD349. The potency of CD349 in inhibiting both types of Ca2+ current was also similar to that of nicardipine. It is suggested that the blocking effect of CD349 on neuronal Ca2+ influx, in combination with a cerebral vasodilatory action, may contribute to a favorable effect on ischemic brain damage. .