2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents.

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Lalloz L, Loppinet V, Coudert G, Guillaumet G, Loubinoux B, Labrid C, Beaughard M, Dureng G, Lamar JC

2-Benzodioxinylaminoethanols: a new class of beta-adrenergic blocking and antihypertensive agents.

J Med Chem. 1981 Aug;24(8):994-8.

PubMed ID

6120237 [ View in PubMed

]

Abstract

Various 2-benzodioxinylaminoethanol derivatives were synthetized and investigated for beta-adrenergic blocking activity. Most compounds demonstrated a beta-blocking activity of a competitive type when evaluated in guinea pig atrial and tracheal preparations. Three compounds were more potent than practolol and propranolol. All compounds demonstrated antihypertensive properties in spontaneously hypertensive rats. The most active compound was 1-(1,4-benzodioxin-2-yl)-2-[N4-(2-methoxyphenyl)piperazino]ethanol (11), which at 2.5 mg/kg iv lowered blood pressure by 41%.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Practolol	Beta-1 adrenergic receptor	Kd (nM)	173.78	N/A	N/A	Details
Propranolol	Beta-1 adrenergic receptor	Kd (nM)	8.71	N/A	N/A	Details