Befunolol HCl

For research use only. Not for therapeutic Use.

  • CAT Number: I023141
  • CAS Number: 39543-79-8
  • Molecular Formula: C16H22ClNO4
  • Molecular Weight: 327.8
  • Purity: 98%
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Befunolol HCl (Cat No.: I023141) is a non-selective beta-adrenergic receptor blocker with intrinsic sympathomimetic activity, primarily used in the treatment of glaucoma and ocular hypertension. It reduces intraocular pressure by decreasing aqueous humor production within the eye. Befunolol offers the advantage of effective pressure control with minimal systemic side effects. Its dual action as a beta-blocker and partial agonist makes it suitable for patients sensitive to other beta-blockers. It is also studied for its cardiovascular effects, particularly in managing mild hypertension and arrhythmias.


CAS Number 39543-79-8
Synonyms

Befunolol HCl; Befunolol hydrochloride; Bentox; BFE 60; BFE-60; BFE60; Glauconex.

Molecular Formula C16H22ClNO4
Purity 98%
Solubility Soluble in DMSO
Appearance Solid powder
Storage Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
IUPAC Name Ethanone, 1-(7-(2-hydroxy-3-((1-methylethyl)amino)propoxy)-2-benzofuranyl)-, hydrochloride
InChI 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
InChIKey TVVTWOGRPVJKDJ-UHFFFAOYSA-N
SMILES CC(C1=CC2=CC=CC(OCC(O)CNC(C)C)=C2O1)=O.[H]Cl
Reference

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3: Reichl S, Müller-Goymann CC. The use of a porcine organotypic cornea construct for permeation studies from formulations containing befunolol hydrochloride. Int J Pharm. 2003 Jan 2;250(1):191-201. PubMed PMID: 12480285.
4: Nino M, Suppa F, Ayala F, Balato N. Allergic contact dermatitis due to the beta-blocker befunolol in eyedrops, with cross-sensitivity to carteolol. Contact Dermatitis. 2001 Jun;44(6):369. PubMed PMID: 11380552.
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6: Koike K, Horinouchi T, Takayanagi I. Comparison of interactions of R(+)- and S(-)-isomers of beta-adrenergic partial agonists, befunolol and carteolol, with high affinity site of beta-adrenoceptors in the microsomal fractions from guinea-pig ciliary body, right atria and trachea. Gen Pharmacol. 1994 Nov;25(7):1477-81. PubMed PMID: 7896063.
7: Maruyama Y, Tanonaka K, Niwa T, Takeo S. Beneficial effects of befunolol on post-hypoxic recovery of cardiac contractility and myocardial metabolism. Arzneimittelforschung. 1992 Dec;42(12):1423-9. PubMed PMID: 1363193.
8: Fusco R, Greco GM, Del Prete A, Caccavale A, Nieto G, Sabbatino S, Santilli F. Long-term effects of befunolol on the corneal endothelium and the consensual ophthalmotonic reaction. Clin Ther. 1992 Nov-Dec;14(6):785-90. PubMed PMID: 1363082.
9: Mancuso G. Allergic contact dermatitis due to befunolol in eyedrops. Contact Dermatitis. 1992 Sep;27(3):198. PubMed PMID: 1360394.
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11: Takayanagi I, Hagiwara H, Koike K, Hosokawa T, Kasuya Y. Effects of the R(+)- and S(-)-isomers of beta-adrenoceptor blockers with intrinsic sympathomimetic activity, befunolol and carteolol, on rabbit intraocular pressure. Can J Physiol Pharmacol. 1991 Aug;69(8):1243-5. PubMed PMID: 1685941.
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13: Maruyama Y, Awaji T, Inoue M, Takeo S. Metabolic profile of beta-adrenoceptor-blocking action of befunolol. Arch Int Pharmacodyn Ther. 1991 May-Jun;311:73-88. PubMed PMID: 1686392.
14: Imamura Y, Nozaki Y, Higuchi T, Otagiri M. Reactivity for prostaglandins and inhibition by nonsteridal anti-inflammatory drugs of rabbit liver befunolol reductase. Res Commun Chem Pathol Pharmacol. 1991 Jan;71(1):49-57. PubMed PMID: 2024065.
15: Höh H. [The local anesthetic effect and subjective tolerance of 0.5% befunolol and 1% pindolol in healthy eyes]. Klin Monbl Augenheilkd. 1990 Apr;196(4):219-24. German. PubMed PMID: 1971855.
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17: Yang L, Zheng JM. [Use of derivative UV spectroscopy to monitor the percutaneous absorption of befunolol-HCL]. Yao Xue Xue Bao. 1990;25(12):916-9. Chinese. PubMed PMID: 2104471.
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19: Takayanagi I, Ogishima M, Koike K. Thermodynamic analysis of beta-adrenergic partial agonists (befunolol and carteolol) interaction with low and high affinity binding sites of beta-adrenoceptors in guinea-pig taenia caecum. Gen Pharmacol. 1990;21(3):303-7. PubMed PMID: 1971246.
20: Imamura Y, Nozaki Y, Otagiri M. Purification and characterization of befunolol reductase from rabbit liver. Chem Pharm Bull (Tokyo). 1989 Dec;37(12):3338-42. PubMed PMID: 2698771.

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