oxprenolol

Names

[ CAS No. ]:
6452-71-7

[ Name ]:
oxprenolol

[Synonym ]:
2-PROPANOL,1-[(1-METHYLETHYL)AMINO]-3-[2-(2-PROPEN-1-YLOXY)PHENOXY]-
Oxprenolol

Biological Activity

[Description]:

Oxprenolol (Ba 39089 free base) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

β-adrenoceptor:7.10 nM (Ki)


[In Vitro]

Oxprenolol is lipophilic[3]. Oxprenolol shows permeability rate constant of 1.54 ± 1.54×10-3 cm/h across abdominal human skin[3].

[In Vivo]

Oxprenolol (200 mg/kg/day; p.o.; daily for 3 weeks) produces effective beta-blockade together with peak plasma drug levels within the normal clinical range[2]. Animal Model: Male rats (230 to 300 g body wt) of the Wistar strain[2] Dosage: 200 mg/kg Administration: Administered orally; daily for 3 weeks Result: This dosage produced effective beta-blockade.

[References]

[1]. T Nagatomo, et al. Binding Characteristics of 3H-dihydroalprenolol to Beta-Adrenoceptors of Rat Heart Treated With Neuraminidase. Jpn J Pharmacol. 1983 Aug;33(4):851-7.

[2]. A S Manning, et al. Abrupt Withdrawal of Chronic Beta-Blockade: Adaptive Changes in Cyclic AMP and Contractility. J Mol Cell Cardiol. 1981 Nov;13(11):999-1009.

[3]. Modamio P, et al. A comparative in vitro study of percutaneous penetration of β-blockers in human skin. International journal of pharmaceutics, 2000, 194(2): 249-259.

Chemical & Physical Properties

[ Density]:
1.0479 (rough estimate)

[ Boiling Point ]:
408.57°C (rough estimate)

[ Melting Point ]:
78-80°

[ Molecular Formula ]:
C15H23NO3

[ Molecular Weight ]:
265.34800

[ Exact Mass ]:
265.16800

[ PSA ]:
50.72000

[ LogP ]:
2.38000

[ Index of Refraction ]:
1.5000 (estimate)

Related Compounds