In vitro assessment for vascular selectivity of a new dihydropyridine derivative, NB-818

Pharmacology and Therapeutic Potential of Lemildipine, a Highly Vasculoselective Dihydropyridine Derivative with Slow Onset and Long Duration of Action

“…Its slow onset of action observed in vivo was confirmed using functional isolated tissue preparations (10). As shown in Fig.…”

“…In rabbit femoral arteries lemildipine antagonized 60 mM K+-induced contractions. In this respect it was about 3 times more potent than nifedipine ( Table 1) (10). On the other hand, lemildipine was much less potent than nifedipine with respect to its negative inotropic effect in guinea pig atria and papillary muscles (10,21).…”

“…In this respect it was about 3 times more potent than nifedipine ( Table 1) (10). On the other hand, lemildipine was much less potent than nifedipine with respect to its negative inotropic effect in guinea pig atria and papillary muscles (10,21). The negative inotropic potency of lemildipine was one-hundredth that of nifedipine (Table 1).…”

“…Lemildipine displayed a slow and long-acting I, , block in guinea pig ventricular cells (10). As illustrated in Fig.…”

Cardiac profile of EGIS-9377, a novel cardiotonic agent as a Ca2+ sensitizer with bradycardiac activity

“…Single ventricular myocytes of the guinea pig were enzymatically isolated using collagenase (0.04% w/v, Wako, Osaka) according to the method described by Tohse (1990). Membrane currents were recorded in the whole-cell voltage-clamp mode of the patch-clamp methods (Hattori et al 1996). The pipette solution contained (in mM): K-glutamate 130, KCl 20, MgCl 2 1.0, Mg-ATP 5.0, Na 2 -GTP 0.1, EGTA 5.0 and HEPES 5.0 (pH 7.4).…”