Ultra-short-acting .beta.-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function

Erhardt, Paul; Woo, C. M.; Anderson, W. Gary; Gorczynski, Richard J.

doi:10.1021/jm00354a003

Cited by 76 publications

(36 citation statements)

References 2 publications

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“…Urethane was used as the anesthetic since it produces long-lasting anesthesia with minimal cardiovascular depression and it does not affect sympathetic outflow appreciably. 13,14 We assume that anesthesia with urethane produced compatible physiological conditions for both landiolol and esmolol.…”

Section: Recording Of Renal Sympathetic Nerve Activity (Rsna)mentioning

confidence: 99%

“…6 Both esmolol and landiolol possess ester bonds in their chemical structure and are hydrolyzed quickly by an esterase in red blood cells, and plasma and liver esterase. 6,14 There are conflicting data regarding the half-life of both agents. Iguchi et al reported that both agents' half-life is approximately nine minutes.…”

Section: Recording Of Renal Sympathetic Nerve Activity (Rsna)mentioning

confidence: 99%

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In rabbits, landiolol, a new ultra-short-acting β-blocker, exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol

Sasao

Tarver

Kindscher

et al. 2001

Can J Anesth/J Can Anesth

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P Pu ur rp po os se e: : To compare the cardiovascular and sympathetic effects of a new ultra-short-acting, highly cardioselective ß-blocker, landiolol, with esmolol, using an in vivo rabbit model. ) were given intravenously, and the effects on heart rate (HR) mean arterial pressure (MAP) and renal sympathetic nerve activity (RSNA) were compared.R Re es su ul lt ts s: : Both landiolol and esmolol produced a dose-dependent decrease in HR. The maximum percent reductions of HR were similar with landiolol 3 mg·kg 1 and esmolol 5 mg·kg 1 (-14.0 ± 0.9% and -13.9 ± 1.4%, mean ± SE, respectively). HR decreased more rapidly with landiolol than with esmolol. Esmolol produced a dose-dependent decrease in MAP that was not observed with landiolol. The percent maximum reduction of MAP was -38.2 ± 3.2% with esmolol 5 mg·kg 1 . RSNA increased in a dose-dependent fashion with esmolol, but no changes were noted with landiolol.C Co on nc cl lu us si io on n: : These results suggest that, in rabbits, landiolol has slightly more potent negative chronotropic action than esmolol with significantly less effects on blood pressure.

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Section: Recording Of Renal Sympathetic Nerve Activity (Rsna)mentioning

confidence: 99%

Section: Recording Of Renal Sympathetic Nerve Activity (Rsna)mentioning

confidence: 99%

In rabbits, landiolol, a new ultra-short-acting β-blocker, exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol

Sasao

Tarver

Kindscher

et al. 2001

Can J Anesth/J Can Anesth

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“…10,13 The ultrashort duration of esmolol is due to the rapid hydrolysis of its alkyl ester link. 13 Landiolol was developed to have better activity and selectivity compared with esmolol.…”

Section: Pharmacological Features Of Landiololmentioning

confidence: 99%

“…10,13 Landiolol was developed in Japan and approved for clinical use in 2002, 9,14,15 which further increased its cardioselectivity and shortened its half-life by replacing the side chain. The cardioselectivity of landiolol is much higher than that of esmolol (β1/β2 =255 vs 33) and its half-life is shorter (4 minutes vs 9 minutes).…”

Section: Introductionmentioning

confidence: 99%

“…The cardioselectivity of landiolol is much higher than that of esmolol (β1/β2 =255 vs 33) and its half-life is shorter (4 minutes vs 9 minutes). 9,10,13,16,17 Landiolol (Corebeta; Ono Pharmaceutical, Osaka, Japan) has been approved as a premedication for coronary CT angiography in Japan since 2011. 18 Landiolol would be an ideal intravenous β-blocker to achieve an optimal image quality in coronary CT angiography.…”

Section: Introductionmentioning

confidence: 99%

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Clinical utility of landiolol for use in coronary CT angiography

Tomizawa¹,

Hayakawa²,

Inoh³

et al. 2015

RRCC

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Although remarkable advancement in computed tomography (CT) has been achieved, heart rate control is important to maintain an optimal image quality in coronary CT angiography. Oral or intravenous β-blockers are used as premedication for this purpose. Landiolol was developed as a β-blocker with very high cardioselectivity (β1/β2 =255) and short half-life (4 minutes). In this review, we report the pharmacological features and usage of landiolol and also its effects on heart rate and image quality in coronary CT angiography. In addition, we discuss the safety of landiolol.

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Soft drug design: General principles and recent applications

2000

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Soft drug design represents a new approach aimed to design safer drugs with an increased therapeutic index by integrating metabolism considerations into the drug design process. Soft drugs are new therapeutic agents that undergo predictable metabolism to inactive metabolites after exerting their therapeutic effect. Hence, they are obtained by building into the molecule, in addition to the activity, the most desired way in which the molecule is to be deactivated and detoxified. In an attempt to systematize and summarize the related work done in a number of laboratories, including ours, the present review presents an overview of the general soft drug design principles and provides a variety of specific examples to illustrate the concepts. A number of already marketed drugs, such as esmolol, remifentanil, or loteprednol etabonate, resulted from the successful application of such design principles. Many other promising drug candidates are currently under investigation in a variety of fields including possible soft antimicrobials, anticholinergics, corticosteroids, β‐blockers, analgetics, ACE inhibitors, antiarrhythmics, and others. Whenever possible, pharmacokinetic and pharmacodynamic properties are briefly summarized and compared to those of other compounds used in the same field. © 2000 John Wiley & Sons, Inc. Med Res Rev, 20, No. 1, 58–101, 2000.

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Ultra-short-acting .beta.-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function

Cited by 76 publications

References 2 publications

In rabbits, landiolol, a new ultra-short-acting β-blocker, exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol

In rabbits, landiolol, a new ultra-short-acting β-blocker, exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol

Clinical utility of landiolol for use in coronary CT angiography

Soft drug design: General principles and recent applications

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