An orally-bioavailable

Oxprenolol (hydrochloride) – 250 mg

Brand:
Cayman
CAS:
6452-73-9
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Oxprenolol is an orally bioavailable β-adrenergic receptor (β-AR) antagonist (Ki = 7.10 nM in a radioligand binding assay using rat heart tissue).{41183} It is non-selective and inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM in isolated rat heart and uterus, respectively).{41184} Oxprenolol is selective for β-ARs over serotonin (5-HT) receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively), but it binds to 5-HT1A receptors in rat hippocampus and 5-HT1B in rat striatum (Kis = 94.2 and 642 nM, respectively).{41185,41186} Formulations containing oxprenolol exhibit some intrinsic sympathomimetic activity and have been used to treat hypertension and angina pectoris.{41187}  

 

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Description

An orally-bioavailable, non-selective β-AR antagonist (Ki = 7.10 nM in rat heart tissue); inhibits both β1- and β2-ARs (Kds = 2.09 and 1.35 nM, respectively, in isolated rat heart and uterus); selective for β-ARs over 5-HT receptors in rat sarcolemmal membrane preparations (IC50s = 4.13 and 23,300 nM, respectively); binds to 5-HT1A and 5-HT1B (Kis = 94.2 and 642 nM, respectively, in rat brain); exhibits some intrinsic sympathomimetic activity

Formal name: 1-[(1-methylethyl)amino]-3-[2-(2-propen-1-yloxy)phenoxy]-2-propanol, monohydrochloride

Synonyms:  dl-Alprenolol|dl-Oxprenolol

Molecular weight: 301.8

CAS: 6452-73-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Angina||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Neuroscience

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