39552-01-7 Usage
Description
Befunolol, a β-adrenergic blocker with intrinsic sympathomimetic action, also functions as a β-adrenergic partial agonist in isolated organs. It is a pharmaceutical compound that has found various applications in the medical field due to its ability to modulate the activity of the sympathetic nervous system.
Uses
Used in Ophthalmology:
Befunolol is used as an antiglaucoma agent in ophthalmic solutions. It helps in reducing intraocular pressure, which is a common issue in glaucoma patients. By acting as a β-adrenergic blocker, it effectively manages the symptoms and prevents further damage to the optic nerve.
Used in Cardiovascular Applications:
As a β-adrenergic blocker, Befunolol is also utilized in the treatment of various cardiovascular conditions. It helps in managing heart rate, blood pressure, and reducing the workload on the heart. This makes it a valuable tool in the management of conditions such as hypertension, angina, and certain arrhythmias.
Used in Isolated Organ Studies:
In research and laboratory settings, Befunolol is used as a β-adrenergic partial agonist in isolated organs. This allows scientists to study the effects of the compound on specific organ systems and gain a better understanding of its mechanisms of action and potential applications in various medical fields.
Originator
Bentos,Kakenyaku Kako,Japan,1983
Manufacturing Process
To 8.8 g of 2-acetyl-7-hydroxybenzofuran were added 80 ml of
epichlorohydrin and 0.2 g of piperidine hydrochloride and the mixture was
heated at 105°C for 3 hours. After the reaction, the excess of epichlorohydrin
was evaporated and the resultant was distilled under reduced pressure to give
9.3 g of 2-acetyl-7-(2,3-epoxypropoxy)benzofuranhaving a boiling point of
175° to 176°C/0.7 mm Hg. 6 g of the product was dissolved in 30 ml of
ethanol and to the solution was added 10 ml of isopropylamine. After refluxing
the mixture for 40 minutes, the solvent was evaporated from the reaction
mixture. The resulting residue was recrystallized from cyclohexane-acetone to
give 6 g of 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy)benzofuran having
a melting point of 115°C.
Therapeutic Function
Beta-adrenergic blocker
Contact allergens
Befunolol was implicated in allergic contact dermatitis
due to beta-blocker agents in eye-drops. Crosssensitivity
has been described with levobunolol.
Check Digit Verification of cas no
The CAS Registry Mumber 39552-01-7 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,9,5,5 and 2 respectively; the second part has 2 digits, 0 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 39552-01:
(7*3)+(6*9)+(5*5)+(4*5)+(3*2)+(2*0)+(1*1)=127
127 % 10 = 7
So 39552-01-7 is a valid CAS Registry Number.
InChI:InChI=1/C16H21NO4/c1-10(2)17-8-13(19)9-20-14-6-4-5-12-7-15(11(3)18)21-16(12)14/h4-7,10,13,17,19H,8-9H2,1-3H3
39552-01-7Relevant 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.
Reaction of Epichlorohydrin with Hydroxybenzofuran
Ohishi, Yoshitaka,Nakanishi, Teruo
, p. 3418 - 3423 (2007/10/02)
Epichlorohydrin (4) was condensed with 2-acetyl-7-hydroxybenzofuran potassium salt (3) to give two radiochemical regio-isomeric 2-acetyl-7-glycidyloxybenzofurans (5a and 5b).The ratio, 5a/5b, was determined to be 5/7 by using 14C-radioisotopic tracer techniques.The present results showed that the reaction proceeds through two different paths in which the phenolate (3) attacks at C-1 of 4 to give 5a and at C-3 to give 5b, the latter path being more favorable than the former.Keywords - epichlorohydrin; nucleophilic substitution; 2-acetyl-7-glycidyloxybenzofuran; radiochemical regio-isomer; 14C-radioisotopic tracer technique; cleavage of carbon chain; reaction mechanism
