BEFUNOLOL HYDROCHLORIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H21NO4.ClH
Molecular Weight	327.803
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=TVVTWOGRPVJKDJ-UHFFFAOYSA-N

InChI=1S/C16H21NO4.ClH/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;1H

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
Assessment of systemic adverse reactions induced by ophthalmic beta-adrenergic receptor antagonists.	2001 Jun	11436944
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
Utilization of 4-chloro-7-nitro-2,1,3-benzoxadiazole (NBD-Cl) for kinetic spectrophotometric assay of befunolol hydrochloride in its pharmaceutical formulation.	2006 May-Jun	16792064
Allergic contact dermatitis due to levobunolol with cross-sensitivity to befunolol.	2007 Jan	17177718
Pharmacological evaluation of ocular beta-adrenoceptors in rabbit by tissue segment binding method.	2009 Jan 30	19087880
Reconstruction of a human cornea by the self-assembly approach of tissue engineering using the three native cell types.	2010 Oct 29	21139684

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 HYDROCHLORIDE

Common Name

English

BFE-60

Code

English

BEFUNOLOL HYDROCHLORIDE [JAN]

Common Name

English

BEFUNOLOL HYDROCHLORIDE [MART.]

Common Name

English

1-(7-(2-HYDROXY-3-((1-METHYLETHYL)AMINO)PROPOXY)-2-BENZOFURANYL)ETHANONE HYDROCHLORIDE

Systematic Name

English

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

Systematic Name

English

Befunolol hydrochloride [WHO-DD]

Common Name

English

BEFUNOLOL HYDROCHLORIDE [MI]

Common Name

English

BEFUNOLOL HCL

Common Name

English

Code System Code Type Description

EVMPD

SUB00686MIG