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

Errors in agonist affinity estimation: do they and should they occur in isolated tissue experiments?

P Leff1, I G Dougall, D H Harper

  • 1Department of Pharmacology, Fisons Research and Development Laboratories, Loughborough, UK.

Trends in Pharmacological Sciences
|February 1, 1990
PubMed
Summary

Agonist affinity measurements may be overestimated by common theories, especially with high intrinsic efficacy. However, accurate constants can be determined if potential errors from these agonist action theories are carefully assessed.

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

β-Blockers have differential effects on the murine asthma phenotype.

British journal of pharmacology·2015
Same author

Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma.

British journal of pharmacology·2012
Same author

Formoterol and salmeterol induce a similar degree of β2-adrenoceptor tolerance in human small airways but via different mechanisms.

British journal of pharmacology·2011
Same author

An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. 1985.

British journal of pharmacology·2010
Same author

Activation of E-prostanoid4 and E-prostanoid2 receptors inhibits TNF-alpha release from human alveolar macrophages.

The European respiratory journal·2007
Same author

Dual dopamine D2 receptor and beta2-adrenoceptor agonists for the treatment of chronic obstructive pulmonary disease: the pre-clinical rationale.

Respiratory medicine·2003

Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Action Mechanisms

Background:

  • Two prominent theories of agonist action, the isomerization and ternary complex mechanisms, suggest potential overestimation of agonist affinity.
  • This overestimation is predicted to be more significant with higher intrinsic efficacy of the agonist.

Purpose of the Study:

  • To evaluate the validity of predictions regarding agonist affinity overestimation by isomerization and ternary complex mechanisms.
  • To determine if experimental data supports the theoretical predictions of error in agonist affinity measurements.
  • To ascertain if accurate agonist affinity constants can be reliably measured despite these theoretical concerns.

Main Methods:

  • Utilizing the inactivation method for measuring agonist affinity.

Related Experiment Videos

  • Comparing theoretical predictions with experimental data to assess accuracy.
  • Implementing strategies to detect and account for potential errors in measurements.

    • Main Results:

    • Theoretical predictions of overestimation in agonist affinity were examined.
    • Experimental data was analyzed to determine the extent to which theoretical predictions hold true.
    • Evidence suggests that accurate agonist affinity constants can be obtained.

    Conclusions:

    • While theories predict potential overestimation of agonist affinity, accurate measurements are achievable.
    • Careful consideration and detection of potential errors, as suggested by theory, are crucial for reliable agonist affinity determination.
    • The study highlights the importance of methodological rigor in pharmacological measurements.