85320-68-9 Usage
Description
Amosulalol, also known by its brand name Lowgan, is a potent antihypertensive medication that combines alpha and beta blocking properties. It is specifically indicated for the treatment of essential hypertension and is known for its minimal side effects. The beta-blocking property of Amosulalol helps to reduce the tachycardia associated with alpha-blockers, while its alpha-blocking activity mitigates the peripheral vasoconstriction that can occur with beta-blockade.
Uses
Used in Pharmaceutical Industry:
Amosulalol is used as an antihypertensive agent for the treatment of essential hypertension. Its dual action in blocking both alpha and beta receptors makes it an effective medication for managing high blood pressure.
Amosulalol is used as a therapeutic agent for reducing tachycardia associated with alpha-blockers. This is due to its beta-blocking property, which helps to counteract the increased heart rate that can occur when alpha-blockers are used.
Amosulalol is also used as a therapeutic agent for reducing peripheral vasoconstriction associated with beta-blockade. Its alpha-blocking activity helps to alleviate the narrowing of blood vessels that can be caused by beta-blockers, thus improving blood flow and overall cardiovascular health.
Manufacturing Process
A mixture of N-benzyl-2-(2-methoxyphenoxy)ethylamine, methyl ethyl ketone,
and 5-bromoacetyl-2-methylbenzenesulfonamide was refluxed with stirring.
After cooling the reaction mixture, ethyl ketone was distilled off under reduced
pressure and the residue formed was dissolved in benzene. Then, ether was
added to the solution and after removing the hydrobromide of N-benzyl-2-(2-
methoxyphenoxy)ethylamine precipitated, the solvent was distilled off under
reduced pressure to provide a viscous oily product.
The viscous oily product was dissolved in ethanol and after adding to the
solution an excess amount of sodium borohydride, the mixture was stirred at
room temperature followed by distilling off ethanol under reduced pressure.
The residue was dissolved in ethyl acetate and the ethyl acetate layer
recovered was washed with water, dried over anhydrous sodium sulfate, and
concentrated under reduced pressure to provide a viscous oily product. The
product was subjected to a silica gel column chromatography and eluted using
benzene and then a mixture of benzene and ethyl acetate of 10:1 by volume
ratio to provide 5-{1-hydroxy-2-[N-benzyl-2-(2-
methoxyphenoxy)ethylamino]ethyl}-2-methyl-benzenesulfonamide as a
viscous oily product.
In 200 ml of methanol was dissolved 20.0 g of 5-{1-hydroxy-2-[N-benzyl-2-
(2-methoxyphenoxy)ethylamino]ethyl}-2-methyl-benzenesulfonamide. After
adding thereto 20 ml of ethanol containing about 10% hydrogen chloride and
1.0 g of 10% palladium charcoal, the mixture was shaken in hydrogen gas
stream. When the absorption of hydrogen stopped, the catalyst was filtered
away and the filtrate was distilled off under reduced pressure. The residue
was dissolved in 100 ml of ethanol while it was hot and the solution was
allowed to stand overnight in ice chamber, whereby 12.8 g of the α-type
crystals of 5-{1-hydroxy-2-[2-(2-methoxyphenoxy)ethylamino]ethyl}-2-
methylbenzenesulfonamide were obtained as the colorless crystals, melting
point 169°-171°C.
In practice it is usually used as monohydrochloride
Therapeutic Function
Alpha-adrenergic blocker, Beta-adrenergic blocker,
Antihypertensive
Check Digit Verification of cas no
The CAS Registry Mumber 85320-68-9 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,5,3,2 and 0 respectively; the second part has 2 digits, 6 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 85320-68:
(7*8)+(6*5)+(5*3)+(4*2)+(3*0)+(2*6)+(1*8)=129
129 % 10 = 9
So 85320-68-9 is a valid CAS Registry Number.
InChI:InChI=1/C18H24N2O5S/c1-13-7-8-14(11-18(13)26(19,22)23)15(21)12-20-9-10-25-17-6-4-3-5-16(17)24-2/h3-8,11,15,20-21H,9-10,12H2,1-2H3,(H2,19,22,23)
85320-68-9Relevant 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.
Drug release controlling coating material for long acting formulations
-
, (2008/06/13)
A coating material for controlling drug release, useful for long acting formulations--e.g. for once-a-day administration, and to a long acting granular composition comprising a drug (especially one conventionally difficult to prepare in long acting form) coated with the coating material. This composition may be mixed with other granular drug formulations. The drug-release controlling coating material comprising, in a specific ratio, one specific water-insoluble and low water-permeability polymers and two materials differing from each other in the pH-dependency of their solubility (pH-dependent polymer-materials).
