5053-06-5 Usage
Originator
Viarespan,Servier,France,1969
Uses
Bronchodilator;anti-adrenergic (β-receptor).
Manufacturing Process
A solution of 192 g of 1-phenethyl-4-hydroxy-4-aminomethyl piperidine in 800
cc of diethylcarbonate is heated for 2? hours to reflux at about 80°C in the
presence of sodium methylate (prepared for immediate use from 2 g of
sodium). After this time, the ethyl alcohol formed during the reaction is slowly
distilled while the maximum temperature is reached. The excess ethyl
carbonate is distilled under reduced pressure. A crystallized residue is then
obtained, which is stirred with 400 cc of water and 400 cc of ether. The
solution is filtered and 125 g (77.6%) of practically pure product melting at
232°C to 233°C, are obtained.The starting material was prepared in a yield of 58% by reduction of the
corresponding cyanohydrin. It in turn was prepared from 1-(2-phenylethyl)-4-
piperidone and potassium cyanide to give the cyanohydrin which was reduced
by lithium aluminum hydride.
Therapeutic Function
Bronchodilator
Pharmaceutical Applications
Fenspiride is an antagonist of 5-hydroxytryptamine, whose effect on bronchial smooth muscle expansion is between isoproterenol and theophylline. It also has the effect of unobtrusion-free respiratory tract and air resistance elimination in the lungs. It has the effect of antitussive, antipyretic, analgesic and anti-inflammatory, and the antipyretic and analgesic effect is better than aminopyrine and the anti-inflammatory effect is stronger than bute.
Check Digit Verification of cas no
The CAS Registry Mumber 5053-06-5 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 5,0,5 and 3 respectively; the second part has 2 digits, 0 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 5053-06:
(6*5)+(5*0)+(4*5)+(3*3)+(2*0)+(1*6)=65
65 % 10 = 5
So 5053-06-5 is a valid CAS Registry Number.
InChI:InChI=1/C15H20N2O2/c18-14-16-12-15(19-14)7-10-17(11-8-15)9-6-13-4-2-1-3-5-13/h1-5H,6-12H2,(H,16,18)
5053-06-5Relevant articles and documents
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.
