Antihypertensive activity of a new calcium channel blocker LF 2.0254, in spontaneously hypertensive rats: a comparison with nifedipine and nicardipine.
LF 2.0254 is a new dihydropyridine calcium channel blocker with a long-lasting antihypertensive action in spontaneously hypertensive rats. In acute experiments, LF 2.0254 was shown to be more potent than nifedipine and nicardipine in reducing blood pressure after i.v. and oral administration with less tachycardia. The hypotensive effects of LF 2.0254 (10 mg/kg) lasted for greater than 24 hr, whereas the blood pressure-lowering effects of nifedipine and nicardipine (10 mg/kg) had disappeared after 6 hr. LF 2.0254 given orally once a day at 10 mg/kg for 14 days to spontaneously hypertensive rats, led to a marked and persistent decrease in blood pressure, with no significant changes in heart rate. In an attempt to prevent the development of hypertension, LF 2.0254 (3 and 10 mg/kg) was given once a day for 8 weeks to 5 week-old SHR. On the last day of treatment, LF 2.0254 had markedly reduced blood pressure over a 24 hr period, however, there was no reduction of left ventricular hypertrophy, since body weight and left ventricular weight were not significantly different between control and treated groups.
Pruneau
D
D
Centre de Recherche, Laboratoires Fournier S.A., Fontaine-lès-Dijon, France.
Brown
N L
NL
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000627:therapeutic use*; D006332:Cardiomegaly / Q000503:physiopathology; D004095:Dihydropyridines / Q000627:therapeutic use*; D006339:Heart Rate / Q000187:drug effects; D006973:Hypertension / Q000188:drug therapy*; D008297:Male; D009529:Nicardipine / Q000627:therapeutic use*; D009543:Nifedipine / Q000627:therapeutic use*; D051381:Rats; D011918:Rats, Inbred SHR; D011921:Rats, Inbred WKY
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C059213:LF 2-0254; D009529:Nicardipine; D009543:Nifedipine