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Predicting compounds that interact with the 2 known agonist-induced conformations of the human β1-adrenoceptor.

The β1-adrenoceptor exists in at least 2 agonist-stabilized conformational ensembles: a "catecholamine" ensemble induced via the intrahelica … ture-activity hypothesis built on the predicted poses CGP12177 and 3 biphasic agonists (alprenolol, oxprenolol, and bucindolol), predictions based on ligand similarity and structural compatibility reasoning were made about 11 other β1-ligands not yet tested for secondary conformation interaction and examined in radioligand binding and functional assays using …

[Use of various preparations with beta-adrenergic blocking action in the overall therapy of thyrotoxicosis].

Three beta-adrenoblockers (trasicor, alpheprol, isoptin) were used in 68 patients with thyrotoxicosis in the complex therapy of the disease. Their effect on hemodynamic indices, urinary catecholamine excretion were studied, and the results of investigation were compared with the data obtained earlier with the use of anaprylin. The action of the latter on the thyroid metabolism was ascertained. Anaprylin proved to be the most effective of the aforementioned preparations. Trasicor, which was somewhat less effective, could be used in patients with thyrotoxicosis complicated by cardiovascular insu

The bovine arterially-perfused eye: an in vitro method for the study of drug mechanisms on IOP, aqueous humour formation and uveal vasculature.

A method is reported in which the isolated bovine eye is perfused through a long posterior ciliary artery with buffered physiological saline … constant flow rate, nor does it alter the permeability of the barrier. Other beta-blockers such as oxprenolol and betaxolol also induce dose-dependent decreases in IOP. By applying a fluorescein dilution technique, it is found that the aqueous formation rate (K(out) = 0.0046 min-1, or 12.9 microliters.min-1) is also reduced by timolol and, in a dose-depende …

Beta-adrenoceptor antagonists and human platelets: relationship of effects to lipid solubility.

Six beta-adrenoceptor antagonists (propranolol (+ and - isomers); ICI-118,551; oxprenolol; timolol; metoprolol; and practolol (+ and - isomers), chosen to represent a spectrum of physicochemical and pharmacological properties, inhibited the response of human platelets to all aggregating agents tested. For any given aggregating agent the extent of inhibition correlated with the lipid solubility of the beta-adrenoceptor antagonist and showed no relation to other properties of these compounds. Inhibition of aggregation by the beta-adrenoceptor antagonists was manifested as a parallel shift to the…

Effects of beta-adrenoceptor antagonists on central haemodynamics in essential hypertension.

1 Eleven β-adrenoceptor blocking agents (propranolol, oxprenolol, penbutolol, carteolol, bupranolol, bufetolol, pindolol, atenolol, metoprolol, acebutolol and labetalol) were orally administered to 144 patients with essential hypertension for 5 weeks to assess their antihypertensive effects. In addition haemodynamic responses were measured non-invasively using radioactive iodinated human serum albumin. 2 In a second study central haemodynamic changes in response to intravenous injection of propranolol (0.4 mg/kg) were assessed in 21 untreated patients with essential hypertension and compared w…

Atypical beta-adrenergic receptor in 3T3-F442A adipocytes. Pharmacological and molecular relationship with the human beta 3-adrenergic receptor.

Expression of ligand binding properties for an atypical beta-adrenergic receptor (beta-AR) subtype was studied during the adipose differenti … nd CHO-beta 3 cells. As in CHO-beta 3 cells, the classical beta 1- and beta 2-antagonists CGP12177, oxprenolol, and pindolol were partial agonists in adipocytes. Although undetectable in preadipocytes, a major mRNA species of 2.3 kilobases (kb) and a minor one of 2.8 kb were observed in adipocytes by hybridization to a human beta 3-AR specific probe.(ABSTRAC …

How intrinsic sympathomimetic activity modulates the haemodynamic responses to beta-adrenoceptor antagonists. A clue to the nature of their antihypertensive mechanism.

1 A survey has been made of the literature on acute and long-term haemodynamic effects of ten different β-adrenoceptor antagonists. The β-adrenoceptor blockers are: pindolol, practolol, alprenolol, oxprenolol, acebutolol, penbutolol, metoprolol, atenolol, propranolol and timolol. The total numbers of patients included in this review are 396 patients in 41 acute studies and 410 patients in 36 long-term studies. 2 The effects of β-adrenoceptor blockers on the concentrations of plasma noradrenaline have also been reviewed. Ten studies including 110 patients on non-ISA-β-adrenoceptor blockers and …

The nifedipine gastrointestinal therapeutic system (GITS). Evaluation of pharmaceutical, pharmacokinetic and pharmacological properties.

Nifedipine is a short-acting calcium antagonist formulated into several different oral preparations, each of which offers a distinct drug re … perhaps leading to less optimal clinical outcomes. For example, the median GI transit time for both oxprenolol and metoprolol Oros drug delivery systems has been reported as 27.4 hours, with individual times ranging from 5.1 to 58.3 hours. The possibility of inadequate GI retention of the nifedipine GITS is perhaps more likely in patients who have pre-existi …

Blood pressure lowering efficacy of partial agonist beta blocker monotherapy for primary hypertension.

BACKGROUND: Partial agonists are a subclass of beta blockers used to treat hypertension in many countries. Partial agonist act by stimulatin … but there was no clear evidence that it lowered DBP. There was no clear evidence that pindolol and oxprenolol lowered SBP or DBP. Other than for celiprolol, sample sizes were generally small increasing the uncertainty in findings for individual agents versus placebo. In patients with moderate to severe hypertension, partial agonists (considered as a subclas …

Repurposing beta-blockers for combinatory cancer treatment: effects on conventional and immune therapies.

Beta-adrenergic receptor signaling regulates cellular processes associated with facilitating tumor cell proliferation and dampening anti-tumor immune response. These cellular processes may lead to compromised tumor control and cancer progression. Based on this ramification, Beta-blockers (BBs) have emerged as a potential treatment by inhibiting beta-adrenergic receptor signaling. This review aimed to investigate the relationship between the use of BBs and tumor progression and treatment response. Therefore, the authors explored several aspects: the potential synergistic relationship of BBs wit

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… Example patients with breast cancer and epithelial ovarian cancer ( Watkins et al., 2015 ; Montoya et al., 2017 ) Carvedilol Nadolol Labetalol Levobunolol Sotalol Timolol Oxprenolol Selective Beta1 blocker (SBB) | Isoprolol | Selective inhibition of β1- receptor | Impact varies: Not as potent as NSBB …

Trial watch: beta-blockers in cancer therapy.

Compelling evidence supports the hypothesis that stress negatively impacts cancer development and prognosis. Irrespective of its physical, biological or psychological source, stress triggers a physiological response that is mediated by the hypothalamic-pituitary-adrenal axis and the sympathetic adrenal medullary axis. The resulting release of glucocorticoids and catecholamines into the systemic circulation leads to neuroendocrine and metabolic adaptations that can affect immune homeostasis and immunosurveillance, thus impairing the detection and eradication of malignant cells. Moreover, catech

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… progression each year in the treated group (95%CI[11%-54%]; p =0.002) | Retrospective | 156 Melanoma | Selective agents: acebutolol, atenolol, betaxolol, bisoprolol, celiprolol, esmolol, metoprolol, nebivolol Non-selective agents: carteolol, carvedilol, labetatol, levobunolol, metipranolol, nadolol, oxprenolol … Significant better response to immunotherapy in the cohort (OR=0.42; 95%CI[0.19–0.94]; p =0.036) and lung cancer subgroup (OR= 0.25; 95%CI [0.08–0.83]); p =0.024) | Meta-analysis | 162 Solid tumors | Acebutolol, atenolol, bisoprolol, carvedilol, celiprolol, labetolol, metoprolol, nadolol, nebivolol, oxprenolol …

Perioperative beta-blockers for preventing surgery-related mortality and morbidity in adults undergoing non-cardiac surgery.

BACKGROUND: Randomized controlled trials (RCTs) have yielded conflicting results regarding the ability of beta-blockers to influence periope … s of beta-blockers were: propranolol, metoprolol, esmolol, landiolol, nadolol, atenolol, labetalol, oxprenolol, and pindolol. In nine studies, beta-blockers were titrated according to heart rate or blood pressure. Duration of administration varied between studies, as did the time at which drugs were administered; in most studies, it was intraoperatively, but …