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

Decrease in penbutolol central response as a cause of changes in its serum protein binding.

R Martínez Jordá1, C Aguirre, R Calvo

  • 1Department of Pharmacology, Faculty of Medicine, Basque Country University, Leioa Bizkaia, Spain.

The Journal of Pharmacy and Pharmacology
|March 1, 1990
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

Efficacy, safety, and tolerability of arbaclofen in Autistic children and adolescents, the AIMS-2-TRIALS-CT1: a randomized, double-blind, placebo-controlled phase II trial.

EClinicalMedicine·2026
Same author

Large-scale analysis of structural brain asymmetries during neurodevelopment: Associations with age and sex in 4265 children and adolescents.

Human brain mapping·2024
Same author

Age influences the efficacy of osteochondral autograft transfer: Promising results for patients under 40.

Revista espanola de cirugia ortopedica y traumatologia·2024
Same author

Age influences the efficacy of osteochondral autograft transfer: Promising results for patients under 40.

Revista espanola de cirugia ortopedica y traumatologia·2024
Same author

Management of cerebral venous thrombosis in Spain: MOTIVATE descriptive study.

Neurologia·2023
Same author

Brain areas activated during visual learning in the cichlid fish Pseudotropheus zebra.

Brain structure & function·2023
Same journal

Farnesoid X receptor blockade attenuates morphological damage, intestinal secretion, and prevents mucus loss induced by SARS-CoV-2 spike protein in the mouse intestine.

The Journal of pharmacy and pharmacology·2026
Same journal

Therapeutic strategies of traditional Chinese medicine for chronic heart failure: from active ingredients to herbal formulations.

The Journal of pharmacy and pharmacology·2026
Same journal

Norisoboldine suppresses epithelial-mesenchymal transition in colorectal cancer by simultaneously inhibiting the CXCR4/CXCR7 chemokine receptors and the JAK/STAT3 signaling pathway.

The Journal of pharmacy and pharmacology·2026
Same journal

Development, characterization, and therapeutic evaluation of uniform dezocine-loaded PLGA microspheres for sustained analgesia and cognitive protection.

The Journal of pharmacy and pharmacology·2026
Same journal

Phytochemical constituents, biological activities, toxicological profiles, and current applications of Muntingia calabura L.: an updated review.

The Journal of pharmacy and pharmacology·2026
Same journal

Uterine relaxant effects of Ageratum conyzoides essential oil: influence of hormonal status and calcium modulation.

The Journal of pharmacy and pharmacology·2026
See all related articles

Inflammation increases alpha 1-acid glycoprotein, which binds more penbutolol (a beta-adrenoceptor antagonist). This reduces the drug's brain uptake and central anticonvulsant effect in diseased mice.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Biochemistry

Background:

  • Penbutolol, a beta-adrenoceptor antagonist, extensively binds to alpha 1-acid glycoprotein (alpha 1-AGP).
  • Alpha 1-AGP levels increase during inflammatory diseases, potentially altering drug binding.
  • Changes in drug binding can affect pharmacokinetics, pharmacodynamics, and therapeutic efficacy.

Purpose of the Study:

  • To investigate the impact of experimental inflammation on penbutolol's central effect and brain uptake.
  • To determine if increased alpha 1-AGP in inflammation affects penbutolol's free fraction and efficacy.

Main Methods:

  • Intravenous administration of penbutolol to mice with experimentally induced inflammation and control mice.
  • Measurement of anticonvulsant response as the central effect of penbutolol.

Related Experiment Videos

  • Quantification of penbutolol brain uptake and free fraction in serum.

    • Main Results:

    • Diseased mice showed a significant decrease in penbutolol's central effect and brain uptake compared to control animals (P < 0.01).
    • A parallel decrease in the free fraction of penbutolol was observed in diseased mice.
    • Results indicate increased serum binding of penbutolol in inflamed conditions.

    Conclusions:

    • Increased alpha 1-AGP concentration in inflammatory diseases leads to higher serum binding of basic drugs like penbutolol.
    • Enhanced binding reduces the free fraction of the drug, consequently diminishing its central pharmacological effect.
    • This highlights the importance of considering inflammatory status in drug therapy involving protein-bound medications.