BEFUNOLOL

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H21NO4
Molecular Weight	291.3422
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)NCC(O)COC1=CC=CC2=C1OC(=C2)C(C)=O

InChI

InChIKey=ZPQPDBIHYCBNIG-UHFFFAOYSA-N

InChI=1S/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

HIDE SMILES / InChI

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/14977495

Befunolol is a beta-adrenergic receptor blocker approved in Japan for the treatment of open-angle glaucoma. The current drug status is unknown.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adrenergic receptor beta 87 Target ID: CHEMBL2094118 Sources: http://www.ncbi.nlm.nih.gov/pubmed/11163052	Antagonist 2778		8.97 null [pKd]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Open-angle glaucoma 51 Sources: http://www.ncbi.nlm.nih.gov/pubmed/11163052	Primary		Approved 8429	BENTOS Approved Use Unknown

PubMed

Title	Date	PubMed
Relationship between caffeine-induced ocular hypertension and ultrastructure changes of non-pigmented ciliary epithelial cells in rats.	1997 Dec	9442454
Aqueous humor dynamics in beagle dogs with caffeine-induced ocular hypertension.	1998 Jun	9673947
Contact dermatitis to topical drugs for glaucoma.	2001 Dec	11753897
Allergic contact dermatitis due to the beta-blocker befunolol in eyedrops, with cross-sensitivity to carteolol.	2001 Jun	11380552
The use of a porcine organotypic cornea construct for permeation studies from formulations containing befunolol hydrochloride.	2003 Jan 2	12480285
[Levels of antiphospholipid antibodies in the serum and aqueous humor of glaucoma patients].	2004	15636221
Human corneal equivalent as cell culture model for in vitro drug permeation studies.	2004 Apr	15031177
Human cornea construct HCC-an alternative for in vitro permeation studies? A comparison with human donor corneas.	2005 Jul	15939241
Pharmacological evaluation of ocular beta-adrenoceptors in rabbit by tissue segment binding method.	2009 Jan 30	19087880

Patents

Sample Use Guides

In Vivo Use Guide

1% solution 2 times daily.

Route of Administration: Other

In Vitro Use Guide

Human cornea construct was used to test befunolol (0,5%) permeability.The permeation coefficient was 9,88*10(-6) cm/s.

Name

Type

Language

BEFUNOLOL

Official Name

English

befunolol [INN]

Common Name

English

Befunolol [WHO-DD]

Common Name

English

7-(2-HYDROXY-3-(ISOPROPYLAMINO)PROPOXY)-2-BENZOFURANYL METHYL KETONE

Systematic Name

English

BEFUNOLOL [MI]

Common Name

English

2-ACETYL-7-(2-HYDROXY-3-ISOPROPYLAMINOPROPOXY)BENZOFURAN

Systematic Name

English

Classification Tree Code System Code

WHO-ATC

S01ED06