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

beta 1-selective adrenoceptor antagonists. 2. 4-ether-linked phenoxypropanolamines.

P J Machin, D N Hurst, R M Bradshaw

    Journal of Medicinal Chemistry
    |November 1, 1983
    PubMed
    Summary

    New beta-blocker compounds selectively target beta 1-adrenoceptors with minimal beta 2-activity. These potent compounds also exhibit partial agonist effects, offering potential therapeutic applications.

    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

    RIFM fragrance ingredient safety assessment, hexyl phenylacetate, CAS Registry Number 5421-17-0.

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association·2019
    Same author

    RIFM fragrance ingredient safety assessment, 2-butanone, CAS Registry Number 78-93-3.

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association·2019
    Same author

    RIFM fragrance ingredient safety assessment, benzenepropanol, α, γ, γ-trimethyl-, CAS Registry Number 2035-93-0.

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association·2019
    Same author

    RIFM fragrance ingredient safety assessment, 5-isopropenyl-2-methyl-2-vinyltetrahydrofuran, CAS registry number 13679-86-2.

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association·2019
    Same author

    RIFM fragrance ingredient safety assessment, 2-nonyn-1-al dimethylacetal, CAS Registry Number 13257-44-8.

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association·2019
    Same author

    RIFM fragrance ingredient safety assessment, hydroxycitronellal dimethyl acetal, CAS Registry Number 141-92-4.

    Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association·2019

    Area of Science:

    • Pharmacology
    • Medicinal Chemistry
    • Cardiovascular Research

    Background:

    • Beta-adrenoceptors play crucial roles in regulating heart rate and blood pressure.
    • Selective beta-1 receptor antagonists are valuable in treating cardiovascular diseases.
    • Developing compounds with high selectivity and specific activity profiles remains a key challenge.

    Purpose of the Study:

    • To synthesize and evaluate a series of novel 4-substituted phenoxypropanolamines.
    • To investigate their selectivity for beta-1 versus beta-2 adrenoceptors.
    • To explore their partial agonist activity and structure-activity relationships.

    Main Methods:

    • Chemical synthesis of 4-substituted phenoxypropanolamines.
    • In vitro assessment of beta-adrenoceptor binding and functional activity.

    Related Experiment Videos

  • Determination of selectivity ratios for beta-1 and beta-2 blockade.
  • Analysis of structure-activity relationships.

    • Main Results:

    • Several compounds, particularly [4-[2-[[2-(4-fluorophenyl)ethyl] oxy]ethoxy]phenoxy]propanolamines (14, 15, and 24), demonstrated potent beta-1 blockade.
    • These compounds exhibited minimal to no beta-2 blockade even at significantly higher doses (>1000-fold).
    • Partial agonist activity was observed for the tested compounds.

    Conclusions:

    • The synthesized phenoxypropanolamines show promising selectivity for beta-1 adrenoceptors.
    • The findings provide insights into the structural requirements for selective beta-adrenoceptor ligand binding.
    • These compounds represent potential leads for developing novel cardiovascular therapeutics.