The current novel corona virus illness (COVID-19) is a developing viral disease that was discovered in 2019. There is currently no viable therapeutic strategy for this illness management. Because traditional medication development and discovery has lagged behind the threat of emerging and re-emerging illnesses like Ebola, MERS-CoV, and, more recently, SARS-CoV-2. Drug developers began to consider drug repurposing (or repositioning) as a viable option to the more traditional drug development method. The goal of drug repurposing is to uncover new uses for an approved or investigational medicine that aren't related to its original use. The main benefits of this strategy are that there is less developmental risk and that it takes less time because the safety and pharmacologic requirements are met. The main protease (Mpro) of corona viruses is one of the well-studied and appealing therapeutic targets. As a result, the current research examines the molecular docking of Mpro (PDB ID: 5R81) conjugated repurposed drugs. 12,432 approved drugs were collected from ChEMBL and drugbank libraries, and docked separately into the receptor grid created on 5R81, using the three phases of molecular docking including high throughput virtual screening (HTVS), standard precision (SP), and extra precision (XP). Based on docking scores and MM-GBSA binding free energy calculation, top three drugs (kanamycin, sulfinalol and carvedilol) were chosen for further analyses for molecular dynamic simulations.

01 Feb 1983·Federation proceedings

Antihypertensive actions of an isomer of labetalol and other vasodilator-beta-adrenoceptor blockers.

Article

Author: Baum, T ; Sybertz, E J

Combinations of beta-adrenoceptor blockers and vasodilators have proved highly useful in antihypertensive therapy. Studies of the mechanisms of action of several agents that combine these effects within a single molecule are described in this report. Labetalol, SCH 19927, sulfinalol, MK-761, pindolol, and prizidilol, in contrast to propranolol, decreased blood pressure of spontaneously hypertensive rats (SHR). All except labetalol and SCH 19927 increased heart rate. In anesthetized dogs, all of these agents (except propranolol) produced vasodilatation on intra-arterial administration into the femoral vascular bed and, given i.v., lowered blood pressure after ganglionic blockade. In contrast to the other agents, labetalol and SCH 19927 caused only minimal increases in heart rate in ganglionically blocked dogs. The vasodilator and hypotensive actions as well as the antihypertensive effect in SHR of labetalol, SCH 19927, sulfinalol, and pindolol were inhibited by propranolol pretreatment but those of prizidilol were not, suggesting that the hypotensive and vascular effects of labetalol, SCH 19927, sulfinalol, pindolol, and MK-761 are mediated by activation of vascular beta-receptors. However, labetalol and SCH 19927 in particular differ from agents of this class as well as other beta blockers with strong intrinsic sympathomimetic actions in that their agonist activity is primarily directed at blood vessels and not the heart.

01 Sep 1982·Archives internationales de pharmacodynamie et de therapie

The pharmacokinetics and pharmacodynamics of sulfinalol hydrochloride in dogs after intravenous administration.

Article

Author: DeFelice, A F ; O'Neil, S K ; Park, G B ; Koss, R F ; Edelson, J

The pharmacokinetic behavior of sulfinalol hydrochloride, an antihypertensive agent with vasodilator and beta-adrenergic blocking activity, was determined in dogs after intravenous administration. The plasma concentrations of sulfinalol HCl were fit to an open two-compartment body model. The mean values for the alpha- and beta-phase constants were 33.3 hr-1 and 0.52 hr-1, respectively. The mean plasma clearance was 2.30 L/kg X hr. The steady-state volume of distribution was approximately four times the body weight of the animals. The urine data gave renal clearance rates approximately equal to the normal glomerular filtration rate in the dog. About 7.5% of the administered dose was excreted in the urine as free sulfinalol hydrochloride. The time course of the hypotensive effect of sulfinalol appears to be better correlated with calculated tissue levels of drug than with observed plasma levels.

100 Deals associated with Sulfinalol

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Indication	Highest Phase	Country/Location	Organization	Date
Hypertension	Discovery	US	Sterling Drug, Inc.	-

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