Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Quantitative structure-activity studies of beta-adrenoceptor blocking drugs to decrease ventricular arrhythmias in

L Gortner1, D Hellenbrecht

  • 1University Children's Hospital, Ulm/Donau, Fed. Rep. of Germany.

Arzneimittel-Forschung
|December 1, 1988
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

[Cystic Fibrosis Screening in Germany].

Klinische Padiatrie·2017
Same author

Superficial Siderosis after Germinal Matrix Hemorrhage.

AJNR. American journal of neuroradiology·2016
Same author

[Child abuse from a pediatric perspective].

Der Radiologe·2016
Same author

Preterm Premature Rupture of Membranes: A Constant Challenge in Perinatal Medicine?

Klinische Padiatrie·2016
Same author

[In Process Citation].

Klinische Padiatrie·2016
Same author

[Specific aspects of pediatric emergencies in the prehospital setting].

Medizinische Klinik, Intensivmedizin und Notfallmedizin·2015
Same journal

Wirksamkeit und Verträglichkeit eines pflanzlichen Arzneimittels mit Kapuzinerkressenkraut und Meerrettich bei akuter Sinusitis, akuter Bronchitis und akuter Blasenentzündung im Vergleich zu anderen Therapien unter den Bedingungen der täglichen Praxis.

Arzneimittel-Forschung·2013
Same journal

Abstracts of the Paul-Martini-Stiftung Symposium 2012 in combination with the National Academy of Leopoldina. November 16-17, 2012. Berlin, Germany.

Arzneimittel-Forschung·2013
Same journal

Leave-one-out procedure in the validation of elimination rate constant analysis.

Arzneimittel-Forschung·2012
Same journal

Pharmacokinetic and myocardial enzyme profiles of two administration routes of epirubicin in breast cancer patients.

Arzneimittel-Forschung·2012
Same journal

Synthesis, anti-hypertensive effect of a novel angiotensin II AT1 receptor antagonist and its anti-tumor activity in prostate cancer.

Arzneimittel-Forschung·2012
Same journal

Effect of zeolite nano-materials and artichoke (Cynara scolymus L.) leaf extract on increase in urinary clearance of systematically absorbed nicotine.

Arzneimittel-Forschung·2012
See all related articles

The lipophilicity of beta-adrenoceptor blockers significantly influences their antiarrhythmic and heart rate-lowering effects. N-alkylation enhances these activities, while ring alkylation shows less consistent impact.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry

Background:

  • Beta-adrenoceptor blocking drugs are crucial in managing cardiac arrhythmias.
  • Understanding the physicochemical properties influencing drug activity is vital for developing effective antiarrhythmic agents.

Purpose of the Study:

  • To investigate the correlation between physicochemical properties, specifically lipophilicity, and the antiarrhythmic activities of phenoxypropanolamine derivatives.
  • To determine the impact of N-alkylation and ring alkylation on drug potency and cardiac effects.

Main Methods:

  • Studied two series of N-alkylated and ring alkylated phenoxypropanolamines.
  • Determined dose-response curves for ventricular arrhythmia threshold (VAT) and heart rate (HR) in anesthetized guinea pigs.
  • Assessed physicochemical properties using n-octanol-buffer partition coefficients (P).

Related Experiment Videos

Main Results:

  • N-alkylation degree positively correlated with increased VAT and decreased HR.
  • Increasing ring alkylation did not consistently enhance biological activity.
  • Statistically significant parabolic correlations were found between hydrophobicity (log P') and biological responses.

Conclusions:

  • The antiarrhythmic and negative chronotropic activities of these beta-blockers are primarily dependent on their lipophilic properties.
  • Steric and pharmacokinetic factors may also play a role in their overall efficacy.