CAS number：132203-70-4
molecular formula：C27H28N2O7
molecular weight：492.52
EINECS number：634-350-6

English synonyms

ATELEC;(+/-)-(e)-cinnamyl 2-methoxyethyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate;O3-(2-Methoxyethyl) O5-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)pyridine-3,5-dicarboxylic acid 3-(2-methoxyethyl)5-[(E)-3-phenyl-2-propenyl] ester;2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid 3-(2-methoxyethyl)5-[(E)-3-phenyl-2-propenyl] ester;Frc 8653,1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methoxyethyl (2E)-3-phenyl-2-propenyl ester;1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic Acid 2-Methoxyethyl (2E)-3-Phenyl-2-propenyl Ester 2-Methoxyethyl (2E)-3-Phenyl-2-propenyl 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate;ilnidipine

Related categories

Pharmaceutical calcium antagonists; ion channels; membrane transport; small molecule inhibitors; antihypertensive; pharmaceutical intermediates; membrane transport/ion channels; calcium antagonists; antiangina drugs; cardiovascular and cerebrovascular drugs; drugs; raw materials; intermediates Body; pharmaceutical raw materials; standard products; traditional Chinese medicine reference substances; pharmaceutical impurities and intermediates; pharmaceutical raw materials; raw materials; chemical raw materials; pharmaceutical raw materials; daily chemicals;
Active Pharmaceutical Ingredients;APIs;Dihydropyridine Class Chemicals;Intermediates & Fine Chemicals;Pharmaceuticals;Calcium channel;Dihydropyridine;API;FRC 8653

Introduction

Hypertension is a common clinical disease, of which essential hypertension accounts for more than 95%, and its pathogenesis has not been fully elucidated. Patients with hypertension have abnormal hemodynamics, accompanied by disorders of fat and glucose metabolism, which can affect the structure and function of important organs such as the heart, brain, and kidneys, and eventually cause organ failure. Safe and effective blood pressure reduction can reduce the disability and mortality of cardiovascular and cerebrovascular diseases. At present, the drugs for the treatment of hypertension are mainly diuretics, angiotensin-converting enzyme inhibitors (ACEI), angiotensin receptor blockers (ARBs), CCBs, and β-receptor blockers. Applications are getting more and more attention.

Chemical properties

Crystallized from methanol with a melting point of 115.5-116.6°C. Acute toxicity LD50 male and female mice, male and female rats (mg/kg): >5000, >5000, >5000, 4412 oral administration; all >5000 subcutaneous injections; 1845, 2353, 441, 426 intraperitoneal injections.

Use

●  Calcium antagonists. For buck.

●  Calcium antagonists. For mild, moderate or severe hypertension, heart failure and ischemic heart disease

●  Cilnidipine is a third-generation dihydropyridine calcium channel blocker, which has a strong blocking effect on both L-type and N-type Ca2+ channels. Animal experiments have shown that it can effectively reduce blood pressure in rats with spontaneous hypertension, boost response caused by acute cold stimulation, and stroke-prone spontaneous hypertension, and can prevent the occurrence of heart, brain, kidney and other organ complications; It also has a significant antihypertensive effect on canine renal hypertension, and there is no rebound phenomenon after drug withdrawal. Human studies have shown that it has a definite antihypertensive effect on essential hypertension, has a weak effect on myocardial contractility, can inhibit the hyperactivity of cardiac sympathetic nerves, does not increase plasma renin activity, and can inhibit the production of norepinephrine and dopamine. Compared with other dihydropyridine calcium channel blockers, this product has the following characteristics:
In addition to acting on the L-type calcium channel like most calcium channel blockers, this product can also act on the N-type calcium channel at the end of the sympathetic nerve, inhibiting the activation of the sympathetic nerve, thus producing unique clinical characteristics. If it does not increase the heart rate of patients with essential hypertension, and can also significantly reduce the patient's cardiothoracic ratio (the ratio of the transverse diameter of the heart to the transverse diameter of the thorax), it is expected to be clinically used to prevent high-risk heart attacks induced by sympathetic reflex activation.
It has good antihypertensive comprehensive curative effect and anti-atherosclerosis effect. Although the antihypertensive activity of this product is similar to that of nifedipine and nicardipine, it has a slow onset of action and a long duration of action. It only needs to be taken once a day, does not increase the heart rate, has weaker inhibition on the myocardium, and has a strong expansion role of the coronary arteries. These comprehensive antihypertensive effects are superior to traditional dihydropyridine calcium channel blockers such as nifedipine. Clinical studies have also shown that this product has anti-atherosclerotic effects while lowering blood pressure, which is manifested by reducing the concentration of lipid peroxidase and the index of atherosclerosis (low-density lipoprotein/high-density lipoprotein cholesterol ), and significantly increased the activity of superoxide dismutase to scavenge oxygen free radicals.

Production method

●  Compound (I) reacts with methyl 3-aminobutenoate to obtain a product.

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