NP 252 Usage And Synthesis

Description

NP-252 is a calcium channel antagonist potentially for the treatment of angina pectoris and congestive heart failure. The vasoinhibitory effects of NP-252 were significantly stronger than those of nifedipine in canine cerebral artery. NP-252 (10(-7) and 10(-6) M) dose-dependently attenuated nifedipine-resistant Ca(++)-contraction in the presence of STA2 in both canine cerebral and coronary arteries. The inhibitory effect of combined treatment with NP-252 (10(-6) M) and nitroglycerin (10(-6) M) on nifedipine-resistant Ca(++)-contraction in the cerebral artery was additive. In aorta, only NP-252 reduced total La3+ resistant 45Ca binding. However, the increases in bound 45Ca at La3+ resistant sites and 45Ca unidirectional influx due to KCl were inhibited by both NP-252 and nifedipine.

Uses

NP-252 is a calcium channel antagonist with an 20% effective dose (ED20) of 2.55 mg/kg in spontaneously hypertensive rats[1].

References

[1] Hojo M, et al. Acute antihypertensive effects of the new generation calcium antagonist 3-pyridine carboxylic acid 5-[(cyclopropylamino)-carbonyl]-1,4-dihydro-2,6-dimethyl-4-(2-nitrophen yl) octyl ester on conscious spontaneously hypertensive rats and renal hypertensive rats. Arzneimittelforschung. 1993 Aug;43(8):847-51. PMID:8216440

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