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-adrenoreceptor blocking heterocyclic oximes and ethers

F Manna1, F Chimenti, A Bolasco

  • 1Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università di Roma La Sapienza, Italy.

Farmaco (Societa Chimica Italiana : 1989)
|November 1, 1996
PubMed
Summary

Researchers synthesized novel heterocyclic compounds to assess their beta-adrenoreceptor blocking activity. While less potent than propranolol in rat hearts, derivatives showed significant beta 2-selectivity in guinea pig trachea, suggesting 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

Implant retention and high rate of treatment failure in hematogenous acute knee and hip prosthetic joint infections.

Medecine et maladies infectieuses·2019
Same author

Five-century record of climate and groundwater recharge variability in southern California.

Scientific reports·2019
Same author

Dermatological manifestations in Noonan syndrome: a prospective multicentric study of 129 patients positive for mutation.

The British journal of dermatology·2018
Same author

Phenolic Plant Extracts Induce Sirt1 Activity and Increase Antioxidant Levels in the Rabbit's Heart and Liver.

Oxidative medicine and cellular longevity·2018
Same author

Distinctive cutaneous and systemic features associated with specific antimyositis antibodies in adults with dermatomyositis: a prospective multicentric study of 117 patients.

Journal of the European Academy of Dermatology and Venereology : JEADV·2017
Same author

[Sulphurous vaginal douching and vulvovaginal atrophy].

La Clinica terapeutica·2017

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Heterocyclic Chemistry

Background:

  • Beta-adrenoreceptors play a crucial role in cardiovascular and respiratory functions.
  • Developing selective beta-adrenoreceptor antagonists is important for treating various conditions.
  • Heterocyclic compounds offer diverse structures for drug discovery.

Purpose of the Study:

  • To synthesize novel thienyl, pyrrol, indolyl, and benzofuryl oxime derivatives and related indole compounds.
  • To investigate the influence of five-membered and condensed heterocyclic substituents on beta-adrenoreceptor inhibiting potency.
  • To evaluate the beta 2-selectivity of the synthesized compounds.

Main Methods:

  • Chemical synthesis of novel heterocyclic oxime and indole derivatives.

Related Experiment Videos

  • In vitro pharmacological evaluation of beta-adrenoreceptor antagonist activity using rat heart and guinea pig trachea preparations.
  • In vivo pharmacological experiments and binding studies to confirm in vitro findings.

    • Main Results:

    • All synthesized heterocyclic derivatives (1-17) demonstrated lower activity than propranolol on rat heart.
    • Compounds exhibited comparable potency to propranolol on guinea pig trachea, showing significant beta 2-selectivity.
    • Lower potency of five-membered heterocyclic derivatives suggests negative influence of oximic carbon polarization on receptor binding.

    Conclusions:

    • The synthesized heterocyclic compounds possess significant beta 2-selective adrenergic antagonist properties.
    • The study provides insights into structure-activity relationships, highlighting the role of heterocyclic substituents and potential interactions with adenyl-cyclase.
    • Findings support the hypothesis of heteroatom interaction with the adenyl-cyclase system, influencing agonist activity.