Disease relevance of Nipradilol

• This beneficial effect suggests that nipradilol should be tested in the patients with portal hypertension [1].
• Effects of nipradilol on myocardial ischaemia produced by coronary stenosis in dogs [2].
• Oral administration of nipradilol and the acute and chronic splanchnic hemodynamic effects of a new beta-blocker with nitrovasodilating properties in patients with liver cirrhosis [3].
• In the presence of LCX stenosis, nipradilol (0.1 mg kg-1, i.v.) produced marked decreases in heart rate and LVdP/dt without a significant increase in left ventricular end-diastolic pressure (LVEDP) [2].
• Nicorandil (5 x 10(-5) and 1.5 x 10(-4) M) or nipradilol (10(-5), 5 x 10(-5) and 1.5 x 10(-4) M) was introduced 5 min before ischemia [4].

High impact information on Nipradilol

• RESULTS: Twice-daily 7-day instillation of nipradilol temporarily but significantly increased human ONH blood velocity, in the ipsilateral eye only (P = 0.005), independent of a reduction in the intraocular pressure [5].
• Topical nipradilol: effects on optic nerve head circulation in humans and periocular distribution in monkeys [5].
• Second, nipradilol or timolol was instilled, and their effects on intravitreal injection of endothelin-1-induced retinal artery contraction were compared, to evaluate whether a pharmacologically active level of nipradilol penetrates the inner limiting layer by topical application [6].
• Coadministration of nipradilol with NMDA reduced cell numbers in the GCL and IPL thickness to 67.8% +/- 2.2% and 74.4% +/- 5.2% of control, respectively (P: < 0.05-0.01) [6].
• PURPOSE: To study the effects of nipradilol, a nonselective beta-blocker with alpha 1-blocking activity and nitroglycerin-like activity, on aqueous humor dynamics and optic nerve head (ONH) circulation in albino rabbits [7].

Chemical compound and disease context of Nipradilol

• These results indicate that nipradilol may have potent hypotensive effects on portal hypertension, similar but not superior to propranolol [8].
• RESULTS: In the nipradilol group, significant preservation of the left ventricular pressure and coronary flow, as well as the level of nitrates and nitrites, was observed, compared with the global ischemia group [9].
• AIMS: To study the effects of topical nipradilol, a non-selective beta blocker with alpha blocking and nitroglycerin-like activities, on intraocular pressure (IOP) and aqueous humour dynamics in normal humans and in patients with ocular hypertension [10].
• Effect of the vasodilatory beta-blocker, nipradilol, and Ca-antagonist, barnidipine, on insulin sensitivity in patients with essential hypertension [11].
• In the area of mild ischemia with MBF of 40-60 ml/min/100 g, nipradilol preserved the tissue ATP and CP levels in spite of a decrease in MBF [12].

Biological context of Nipradilol

• Nipradilol (12 mg/dag, n = 12) significantly diminished wedged hepatic venous pressure (WHVP, 25 +/- 16%), the hepatic venous pressure gradient (HVPG, 20 +/- 12%), and estimated hepatic blood flow (EHBF, 18 +/- 16%) [8].
• Thus, the marked reduction of portal pressure after nipradilol administration depends in part on a limited increase in hepatocollateral resistance [1].
• When nonresponders were excluded, there was a significant correlation of the percentage of reduction between WHVP and CI or systemic vascular resistance, in the nipradilol group [8].
• Pulmonary capillary wedge pressure and central venous pressure, an index of preload, were decreased slightly in the nipradilol group [8].
• Nipradilol produced no significant effect on outflow facility to general blood circulation, whereas it substantially increased uveoscleral outflow [7].

Anatomical context of Nipradilol

• Propranolol, but not nipradilol significantly increased hepatocollateral resistance in cirrhotic rats but not in portal vein stenosed rats [1].
• Single instillation of 0.25% nipradilol showed no significant effect on blood-aqueous barrier permeability and decreased aqueous flow rate in the treated eye (17%; P < 0.01) and in the contralateral eye (9%, P < 0.05) [7].
• Axonal regeneration of cat retinal ganglion cells is promoted by nipradilol, an anti-glaucoma drug [13].
• Some effects of nipradilol, a beta-antagonist possessing a nitroxy group, on smooth muscle of the pig coronary artery [14].
• However, improvement by these two agents of regional dysfunction in the ischaemic myocardium was comparable to those seen with nipradilol [2].

Associations of Nipradilol with other chemical compounds

• The percentage of portal pressure reduction and the frequency of nonresponders did not differ between the nipradilol and propranolol groups [8].
• Effects of nicorandil and nipradilol on ischemic myocardium in perfused rat heart [4].
• Treatment of cortical cultures with a high concentration (500 microM) of nipradilol significantly reduced cell viability, increased lactate dehydrogenase (LDH) release and nitrite concentration in culture medium, whereas desnitro-nipradilol (3,4-dihydro-8-(2-hydroxy-3-isopropylamino)propoxy-3-hydroxy-2H-1-benzopyran) had no significant effects [15].
• Varying concentrations of two NO donors, sodium nitroprusside (SNP) and nipradilol, were added to medium with or without an NO scavenger, a soluble guanylyl cyclase inhibitor, or a PKG inhibitor [16].
• Compared with control, infarct size was reduced by ischemic preconditioning (26%+/-4% versus 49%+/-3%, IPC versus control; p<0.01), L-arginine (24%+/-2%; p<0.01 versus control), and nipradilol (24%+/-2%; p<0.01 versus control) [17].

Gene context of Nipradilol

• Increase of NO metabolites, protein and mRNA of eNOS was also partially inhibited by co-treatment of NOS inhibitor, L-NA with nipradilol [18].
• Nipradilol down-regulated Bax gene expression 12 hr after serum deprivation, and that of the capase-9 and Smac/DIABLO genes at 24 hr, compared to the serum-free sample, while it also increased cell viability and decreased DNA ladder formation at 48 hr [19].
• Effects of nipradilol, a nitric oxide-releasing beta-adrenoceptor blocking agent, on phosphoenolpyruvate carboxykinase gene transcription in a rat hepatoma cell line [20].
• RESULTS: Retinal arterial blood flow and the diameter of the retinal artery significantly (p< 0.05) increased at 4 hours after instillation in nipradilol-treated eyes [21].
• Nipradilol (3,4-dihydro-(2-hydroxy-3-isopropylamino)-propoxy-3-nitroxy-2H-1- benzopyran, K-351, CAS 81486-22-8) is a new type of beta-blocker with vasodilating action [22].

Analytical, diagnostic and therapeutic context of Nipradilol

• RESULTS: Unilateral topical administration of 0.25% nipradilol solution lowered intraocular pressure (IOP) with relatively weak contralateral effects in a dose-dependent manner with a maximum reduction of 6 mm Hg and an effect duration of 6 hours [7].
• 1. The effects of nipradilol, a beta-adrenoceptor antagonist which possesses a nitroxy group, on cytosolic Ca2+ concentration ([Ca2+]i), and on tension development were simultaneously measured by front-surface fluorometry and fura-2-loaded strips in the proximal portion of pig coronary arteries [14].
• Here we show that an anti-glaucoma drug, nipradilol, at low concentration led to a four-fold increase in the number of cat retinal ganglion cells regenerating their axons into a transplanted peripheral nerve 4 and 6 weeks after axotomy [13].
• Only nipradilol preserved peak developed pressure during reperfusion [17].
• However, in the nipradilol plus ischemic preconditioning group, the protective effects were eliminated [9].

References