ICI141292 - CAS 86880-51-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H23N3O4
Molecular Weight:
369.41
COA:
Inquire
Targets:
Adrenergic Receptor
Description:
ICI141292, also known as Epanolol, is a adrenergic β-antagonist with a greater affinity for β1- than β2-adrenoceptors, which is used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
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Synonyms:
N-[2-[[3-(2-cyanophenoxy)-2-hydroxypropyl]amino]ethyl]-2-(4-hydroxyphenyl)acetamide; epanolol; ICI 141,292; ICI 141292; ICI-141,292; N-(2-((3-(2-cyanophenoxy)-2-hydroxypropyl)amino)ethyl)-4-hydroxyphenylacetamide; Visacor
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
689.7±55.0 ℃ at 760 Torr
Melting Point:
118-120 ℃
Density:
1.28±0.1 g/cm3
InChIKey:
YARKMNAWFIMDKV-UHFFFAOYSA-N
InChI:
1S/C20H23N3O4/c21-12-16-3-1-2-4-19(16)27-14-18(25)13-22-9-10-23-20(26)11-15-5-7-17(24)8-6-15/h1-8,18,22,24-25H,9-11,13-14H2,(H,23,26)
Canonical SMILES:
C1=CC=C(C(=C1)C#N)OCC(CNCCNC(=O)CC2=CC=C(C=C2)O)O
1.Long-term hemodynamic effects at rest and during exercise of newer antihypertensive agents and salt restriction in essential hypertension: review of epanolol, doxazosin, amlodipine, felodipine, diltiazem, lisinopril, dilevalol, carvedilol, and ketanserin.
Omvik P1, Lund-Johansen P. Cardiovasc Drugs Ther. 1993 Apr;7(2):193-206.
Hypertension is due to disturbance of the complex interplay between numerous known and unknown mechanisms that normally control blood pressure. Antihypertensive agents may, therefore, reduce blood pressure through widely different actions and, at the same time, elicit counterregulatory responses. This is a review of the long-term hemodynamic effects at rest as well as during exercise of nine relatively new antihypertensive compounds: a beta-blocker (epanolol), an alpha-receptor blocker (doxazosin), two double-acting compounds (dilevalol and carvedilol), three calcium antagonists (amlodipine, felodipine, and diltiazem), an angiotensin-converting enzyme inhibitor (lisinopril), a serotonin antagonist (ketanserin), and low-salt diet as a nonpharmacological treatment in 171 patients with mild to moderate essential hypertension. The results in the treatment groups are compared to the hemodynamic changes seen in 28 hypertensive patients left untreated for 10 years.
2.Effect of beta-adrenoceptor blockade on atrial natriuretic peptide levels during exercise in angina pectoris.
Riley M1, Elborn JS, Onuoha G, Erwin C, Shaw C, Khan MM, Stanford CF, Nicholls DP. Br J Clin Pharmacol. 1993 Feb;35(2):209-12.
The effects of epanolol (200 mg once daily) and diltiazem (60 mg three times daily) on the response of atrial natriuretic peptide (ANP) to exercise were investigated in a double-blind placebo-controlled crossover study in 16 patients with angina pectoris. Exercise tolerance as assessed by peak oxygen consumption was similar with all treatments. Peak heart rate (mean and 95% confidence intervals) was lower (P < 0.05) with epanolol (121 (115-130) beats min-1) than with diltiazem (137 (126-148) beats min-1) or placebo (141 (130-152) beats min-1). ANP did not change from resting values with placebo or diltiazem, but rose significantly (P < 0.05) with epanolol from 19.7 (13.0-29.8) pg ml-1 (geometric mean and 95% confidence intervals) during supine rest to 49.6 (33.7-73.0) pg ml-1 at peak exercise. Since ANP release is stimulated by atrial distension, patients with untreated angina may stop exercise before atrial dilatation occurs. With beta-adrenoceptor blockade, a reduction in peak heart rate may necessitate increased chamber volumes to maintain cardiac output, accounting for the rise in ANP.
3.Comparative effects of epanolol and diltiazem on exercise performance and respiratory gas exchange in angina pectoris.
Riley M1, Elborn JS, Khan MM, Stanford CF, Nicholls DP. Eur Heart J. 1992 Aug;13(8):1116-22.
The effects of epanolol (a new selective beta-adrenoceptor antagonist), diltiazem and placebo were compared in a group of 16 patients with chronic stable angina pectoris. Each patient received each treatment in random order. Diltiazem reduced weekly angina attack rate from 7.2 (95% CI 3.9-10.5) to 3.9 (1.9-5.9) (P less than 0.01), whereas a lesser reduction was observed after epanolol. Both drugs produced a small but significant (P less than 0.05) increase in treadmill exercise time (placebo 474 s (374-574), epanolol 527 s (431-623) and diltiazem 554 s (462-646). However, aerobic work capacity, assessed by peak achieved oxygen consumption, was not different from the placebo value of 21.2 (18.0-24.4) ml.min-1.kg-1, and clearly subnormal when compared to age- and sex-matched controls (33.0 (30.1-35.9) ml.min-1.kg-1). Ventilatory abnormalities and increased lactate levels on active treatment were observed at peak exercise only. We conclude that the cardiodepressant effects of both active drugs limit blood supply to working skeletal muscle, and that chest pain may be replaced by dyspnoea or fatigue as the limiting factors to exercise.
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CAS 86880-51-5 ICI141292

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