AbstractA new method for the quantitative enantiospecific determination of rac‐brefanolol, a vasodilating β‐adrenoceptor blocking agent, in human plasma is described. After an alkaline liquid‐liquid extraction from biological material and a preseparation on a silica gel column with fractional collection of the eluate, the separation of the underivatized enantiomers is performed by high‐performance liquid chromatography on cellulose tris‐4‐methylbenzoic acid polymer coated on silica gel. The UV‐absorbance of the eluate was monitored at 254 nm. Determination limits are 10 ng enantiomer per ml plasma and allow the performance of pharmacokinetic studies after the aimed therapeutic dosages.

01 Jul 1990·Journal of Cardiovascular PharmacologyQ4 · MEDICINE

Hemodynamic Effects of Brefanolol and Propranolol Assessed by Noninvasive Methods in Patients with Arterial Hypertension

Q4 · MEDICINE

Article

Author: Halabi, I ; Halabi, A ; Endell, W ; Kirch, W

In a placebo-controlled, randomized, cross-over study, 16 patients (10 males, 6 females; 50.6 +/- 10.4 years; body weight of 74.5 +/- 8.9 kg; mean +/- SD) with arterial hypertension (WHO stages I and II) were administered single oral doses of placebo, 80 mg of propranolol, as well as 50 and 100 mg of brefanolol (a beta-adrenergic blocking agent with vasodilating properties) in order to determine the resulting hemodynamic effects. Blood pressure, heart rate, and various hemodynamic parameters were assessed noninvasively by mechano- and impedance cardiography as well as by venous occlusion plethysmography before and 2, 4, 6, 10, and 24 h after drug administration. Treatment with propranolol resulted in the typical hemodynamic changes induced by a beta-adrenergic blocking agent characterized by a significant reduction in blood pressure, heart rate, cardiac output, stroke volume, and an increase in total peripheral resistance. A dose of 100 mg of brefanolol also led to comparable hemodynamic effects. Similar significant decreases in blood pressure, heart rate, and cardiac output also occurred with 50 mg of brefanolol, but stroke volume and reactive hyperemia increased. Thus, in this phase of drug development, dose titration with 50 and 100 mg of brefanolol indicates that the lower dose gives rise to a more balanced relationship between its beta-adrenergic blocking and vasodilating properties.

Turkish Journal of Biology

Virtual drug repurposing study against SARS-CoV-2 TMPRSS2 target

Author: Durdagi, Serdar

Currently, the world suffers from a new coronavirus SARS-CoV-2 that causes COVID-19.Therefore, there is a need for the urgent development of novel drugs and vaccines for COVID-19.Since it can take years to develop new drugs against this disease, here we used a hybrid combined mol. modeling approach in virtual drug screening repurposing study to identify new compounds against this disease.One of the important SARS-CoV-2 targets namely type 2 transmembrane serine protease (TMPRSS2) was screened with NPC′s NIH small mol. library which includes approved drugs by FDA and compounds in clin. investigation.We used 6654 small mols. in mol. docking and top-50 docking scored compounds were initially used in short (10-ns) mol. dynamics (MD) simulations.Based on average MM/GBSA binding free energy results, long (100-ns) MD simulations were employed for the identified hits.Both binding energy results as well as crucial residues in ligand binding were also compared with a pos. control TMPRSS2 inhibitor, Camostat mesylate.Based on these numerical calculations we proposed a compound (benzquercin) as strong TMPRSS2 inhibitor.If these results can be validated by in vitro and in vivo studies, benzquercin can be considered to be used as inhibitor of TMPRSS2 at the clin. studies.

100 Deals associated with Brefanolol

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KEGG	Wiki	ATC	Drug Bank
-	Brefanolol	-	-

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Indication	Highest Phase	Country/Location	Organization	Date
Angina Pectoris	Phase 2	Germany	Beiersdorf AG	-
Arrhythmias, Cardiac	Phase 2	Germany	Beiersdorf AG	-
Hypertension	Phase 2	Germany	Beiersdorf AG	-

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