132203-70-4 Usage
Description
Cilnidipine is a dihydropyridine calcium channel blocker, a novel calcium antagonist with the blocking effect on both L-type and N-type calcium channels. It is characterized by its yellow crystalline solid appearance and is used primarily for the treatment of hypertension. Cilnidipine's unique ability to block both N-type and L-type calcium channels allows it to dilate both arterioles and venules, reducing capillary bed pressure and attenuating platelet activation associated with catecholamines. It is well-tolerated with low toxicity and has demonstrated efficacy in various applications, including cell viability assays, photoirradiation and photodegradation studies, and as an antihypertensive agent.
Uses
Used in Pharmaceutical Industry:
Cilnidipine is used as an antihypertensive agent for the treatment of essential and severe hypertension, as well as hypertension associated with renopathy. It exerts a potent vasodilating effect by blocking calcium influx via dihydropyridine-sensitive, voltage-dependent calcium channels, making it superior for long-term treatment due to its slow onset and long duration with less cardiodepressant activity.
Used in Research Applications:
Cilnidipine is used in cell viability assays of pheochromocytoma (nPC12) cells to study its effects on cell function and viability. It is also utilized in photoirradiation and photodegradation studies to understand its impact on albuminuria in diabetic nephropathy, providing valuable insights into its potential therapeutic applications in renal conditions.
Used in Neuroprotection:
Cilnidipine is used in a rat model of focal brain ischemia, where it has been shown to reduce the cerebral infarction area at a dosage of 100 μg/kg, indicating its potential neuroprotective properties.
Used in Cardiology:
Cilnidipine may also be useful in ischemic heart disease, as it has been demonstrated to reduce mean blood pressure and cerebral vascular resistance without affecting cerebral blood flow in anesthetized rats at doses ranging from 3-100 μg/kg.
Brand Names:
Cilnidipine is marketed under various brand names, including Cinalong, Siscard, and Atelec, making it accessible for patients requiring treatment for hypertension and related conditions.
References
https://www.drugbank.ca/drugs/DB09232
https://en.wikipedia.org/wiki/Cilnidipine
Biological Activity
Dual L- and N-type calcium channel blocker that displays antihypertensive, sympatholytic and neuroprotective activity. Lowers mean blood pressure and reduces the size of cerebral infarction in the rat model of focal brain ischemia.
Biochem/physiol Actions
Cilnidipine is a slow-acting Ca2+ channel blocker; antihypertensive; vasodilator; dual blocker of L-type voltage-gated Ca2+ channels in vascular smooth muscle and N-type Ca2+ channels in sympathetic nerve terminals that supply blood vessels. Cilnidipine may offer an advantage over nifedipine as the long term intake of the latter has been linked to increased risk of myocardial infarction and mortality in patients with coronary artery disease. Cilnidipine lowers blood pressure, but has less effect on sympathetic activity. Unlike nifedipine, cilnidipine does not inhibit PKC.
Check Digit Verification of cas no
The CAS Registry Mumber 132203-70-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,2,2,0 and 3 respectively; the second part has 2 digits, 7 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 132203-70:
(8*1)+(7*3)+(6*2)+(5*2)+(4*0)+(3*3)+(2*7)+(1*0)=74
74 % 10 = 4
So 132203-70-4 is a valid CAS Registry Number.
InChI:InChI=1S/C27H28N2O7/c1-18-23(26(30)35-14-8-11-20-9-5-4-6-10-20)25(21-12-7-13-22(17-21)29(32)33)24(19(2)28-18)27(31)36-16-15-34-3/h4-13,17,25,28H,14-16H2,1-3H3/b11-8+
132203-70-4Relevant articles and documents
Preparation method of cilnidipine
-
Paragraph 0026; 0051-0056; 0063-0074; 0076, (2021/02/20)
The invention relates to a preparation method of cilnidipine. The invention provides a preparation method of cinnamyl 3-aminobut-2-enoate, which comprises the following step: carrying out amination reaction on cinnamyl acetoacetate and ammonium carbonate to obtain the cinnamyl 3-aminobut-2-enoate. On the basis, the invention further provides a method for preparing cilnidipine by taking the cinnamyl 3-aminobut-2-enoate as a raw material. The method provided by the invention is relatively low in reaction temperature, relatively short in reaction time, relatively high in product yield and purity,and simple in aftertreatment.
Cilnidipine preparation method
-
Paragraph 0084-0100, (2016/10/07)
The invention provides a cilnidipine preparation method. The method includes the steps that 2-(3-nitrophenyl methylidene) methoxyethyl acetoacetate and 3-amino-2-butenoic acid cinnamyl ester serve as reaction raw materials and react under catalysis of concentrated hydrochloric acid to obtain cilnidipine. A common inorganic catalyst is adopted in the method for catalysis reaction so that reaction time can be effectively shortened; besides, quality of a crude product is high, the yield is high, and cilnidipine has metallic luster. The requirement for refining of reaction is low. Purity of the crude product is good, and the quality requirement can be basically met through one time of refining. The technology is reasonable in design, purity of the refined cilnidipine product is high, and the quantity of any impurity and total impurities is small.
