75530-68-6 Usage
Description
Nilvadipine is a new, second-generation calcium channel blocker effective in the
treatment of hypertension and angina pectoris. Its potent inhibitory effect on the
stimulated chemotaxis of smooth muscle cells and protective action against calcium
deposition suggest that nilvadipine may be useful for preventing and treating
atherosclerosis.
Originator
Fujisawa (Japan)
Uses
Different sources of media describe the Uses of 75530-68-6 differently. You can refer to the following data:
1. Used as an antihypertensive and antianginal.
2. Used as an antihypertensive and antianginal
Manufacturing Process
To a solution of isopropyl ester of 6-formyl-5-methoxycarbonyl-2-methyl-4-(3-
nitrophenyl)-1,4-dihydropyridine- 3-carboxylic acid (4.5 g) in acetic acid (35
ml) were added hydroxylamine hydrochloride (0.97 g) and sodium acetate
(1.43 g), and the mixture was stirred at ambient temperature for 2.5 hours.
After acetic anhydride (4.14 g) was added to this reaction mixture, the
mixture was stirred at ambient temperature for 1.5 hours and at 95-100°C for
additional 4 hours. The acetic acid and the excess of acetic anhydride were
removed in vacuum, followed by adding water to the residue and it was
neutralized with a saturated aqueous solution of sodium bicarbonate. This
aqueous suspension was extracted twice with ethyl acetate, and the combined
extract was washed with water, dried over anhydrous magnesium sulfate and
evaporated to dryness under reduced pressure to give a reddish-brown oil
(4.88 g), which was chromatographed over silica gel (150 g) with a mixture of benzene and ethyl acetate (10:1 by volume) as an eluent to give a crude
crystals (2.99 g). These were recrystallized from ethanol to give yellow prisms
(1.89 g) of isopropyl ester of 6-cyano-5-methoxycarbonyl-2-methyl-4-(3-
nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid melting point 148-150°C
(yellow prisms from ethanol); [α]D20 = 222.4° (c = 1 in methanol).
Brand name
Nivadil
Therapeutic Function
Calcium entry blocker, Antihypertensive
References
1) Paris?et al. (2014),?The spleen tyrosine kinase (Syk) regulates Alzheimer amyloid-β production and Tau hyperphosphorylation; J. Biol. Chem.,?289?33927
2) Rosenthal (1994),?Nilvadipine: profile of a new calcium antagonist. An overview; J. Cardiovasc. Pharmacol. 24 Suppl 2?S92
3) Nimmrich and Eckert (2013),?Calcium channel blockers and dementia; Br. J. Pharmacol.?169?1203
4) Otori?et al. (2003),?Protective effect of nilvadipine against glutamate neurotoxicity in purified retinal ganglion cells; Brain Res.?961?213
Check Digit Verification of cas no
The CAS Registry Mumber 75530-68-6 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,5,5,3 and 0 respectively; the second part has 2 digits, 6 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 75530-68:
(7*7)+(6*5)+(5*5)+(4*3)+(3*0)+(2*6)+(1*8)=136
136 % 10 = 6
So 75530-68-6 is a valid CAS Registry Number.
InChI:InChI=1/C19H21N3O6/c1-10(2)28-19(24)15-11(3)21-14(9-20)17(18(23)27-4)16(15)12-6-5-7-13(8-12)22(25)26/h5-8,10-11,15-16,21H,1-4H3
75530-68-6Relevant articles and documents
METHODS FOR TREATING CHRONIC FATIGUE SYNDROME AND MYALGIC ENCEPHALOMYELITIS
-
, (2021/03/13)
In one aspect the invention relates to a method of treatment selected from the group consisting of: (a) treating a symptom such as pain in a subject identified or diagnosed as having Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS); (b) treating a symptom such as pain in a subject having dysfunctional TRPM3 ion channel activity; (c) restoring NK cell function in a subject having dysfunctional TRPM3 ion channel activity; and (d) restoring calcium homeostasis in a subject having dysfunctional TRPM3 ion channel activity. The method comprises the step of administering to the subject a therapeutically effective amount of at least one therapeutic compound selected from the group consisting of: (i) an opioid receptor antagonist; (ii) an opioid antagonist; and (iii) a therapeutic compound that restores TRPM3 ion channel activity. In some embodiments the therapeutic compound is naltrexone hydrochloride.
THERAPY FOR COMPLICATIONS OF DIABETES
-
, (2009/07/02)
A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
Method for treating resistant hypertension
-
, (2008/06/13)
A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.
