Search results for "Beta-adrenergic blocking agent"
showing 4 items of 4 documents
Beta-adrenergic blocking activity and haemodynamic effects in man of K� 1313, a new beta-adrenergic antagonist
1971
The beta-adrenergic blocking activity and haemodynamic effects of o-[2-hydroxy-3-(isopropylamino)-propoxy]-benzonitril (Ko 1313) have been studied in 22 patients. Antagonism of isoproterenol-induced tachycardia was used as a measure of the beta-adrenergic blocking activity. Ko 1313 1.0 mg had its maximum beta-adrenoceptor blocking effect 5–30 min after intravenous injection. Ko 1313 10.0 mg produced maximum betablockade 1–4 h after oral administration. 1.0 mg Ko 1313 injected intravenously had approximately the same beta-adrenergic blocking effect as 1.0 mg propranolol also given intravenously. After intravenous administration Ko 1313 was 3–4 times as potent as the same dose given orally. A…
Beta-blockers: Historical Perspective and Mechanisms of Action
2019
Beta-blockers are widely used molecules that are able to antagonize β-adrenergic receptors (ARs), which belong to the G protein-coupled receptor family and receive their stimulus from endogenous catecholamines. Upon β-AR stimulation, numerous intracellular cascades are activated, ultimately leading to cardiac contraction or vascular dilation, depending on the relevant subtype and their location. Three subtypes have been described that are differentially expressed in the body (β1-, β2- and β3-ARs), β1 being the most abundant subtype in the heart. Since their discovery, β-ARs have become an important target to fight cardiovascular disease. In fact, since their discovery by James Black in the …
A comparison of the antihypertensive action of propranolol and the optical isomers of N-isopropyl-p-nitrophenylethanolamine (INPEA)
1969
In hypertensive patients, the effect of propranolol and of the optical isomers of N-isopropyl-p-nitrophenylethanolamine (INPEA) on blood pressure was studied. Single oral doses of 40 mg propranolol, 700 mg (−)-INPEA and 700 mg (+)-INPEA decreased supine systolic as well as standing systolic and diastolic blood pressure. Single intravenous doses of 75 mg (−)-INPEA and 75 mg (+)-INPEA lowered supine systolic and diastolic blood pressure. The antihypertensive action of the beta adrenergic blocking levorotatory isomer of INPEA and of the dextrorotatory isomer, which is devoid of beta adrenergic blocking activity, did not differ. It is concluded from these results that the antihypertensive actio…