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

8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist.

R A Bakker1, D M Weiner, T ter Laak

  • 1Leiden/Amsterdam Center for Drug Research, Department of Medicinal Chemistry, Vrije Universiteit Amsterdam, Amsterdam, The Netherlands. ra.bakker@few.vu.nl

Molecular Pharmacology
|February 24, 2004
PubMed
Summary

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

Olanzapine as an add-on, pre-operative anti-emetic drug for postoperative nausea or vomiting: a randomised controlled trial.

Anaesthesia·2023
Same author

Oral cholera vaccination promotes homing of IgA<sup>+</sup> memory B cells to the large intestine and the respiratory tract.

Mucosal immunology·2018
Same author

Leukotriene cysLT1 (LTD4) receptor antagonism of H1-antihistamines: An in vitro study.

Inflammation research : official journal of the European Histamine Research Society ... [et al.]·2016
Same author

A new method for the determination of partition coefficients of air sensitive copper(i) complexes.

Pharmaceutical research·2013
Same author

Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors.

Diabetes, obesity & metabolism·2011
Same author

Feasibility and preliminary effectiveness of preoperative therapeutic exercise in patients with cancer: a pragmatic study.

Physiotherapy theory and practice·2010

Researchers discovered 8R-lisuride, a potent partial agonist for the human histamine H1 receptor (H1R). This finding offers a new tool for studying H1R activity and potential therapeutic applications beyond allergy treatments.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Discovery

Background:

  • The human histamine H1 receptor (H1R) is a key target for allergy medications.
  • While H1R antagonists are common, the effects and utility of H1R agonists are less understood.
  • Neuropsychiatric drugs often antagonize H1R, causing side effects.

Purpose of the Study:

  • To investigate the potential of H1R agonism.
  • To screen known therapeutics and reference drugs for H1R agonist activity.
  • To identify novel compounds with H1R agonist properties.

Main Methods:

  • Utilized a cell-based functional assay to screen compounds.
  • Evaluated H1R agonist activity using receptor selection and amplification technology, inositol phosphate accumulation, and NF-κB activation assays.

Related Experiment Videos

  • Employed H1R mutants and molecular modeling to investigate ligand binding.

    • Main Results:

    • Identified three ergot-based compounds with previously unknown H1R agonist activity.
    • 8R-lisuride demonstrated potent stereospecific partial agonist activity across multiple assays (pEC50 values ~7.9-8.1).
    • Molecular modeling indicated that lisuride binds to a pocket similar to histamine's binding site on the H1R.

    Conclusions:

    • 8R-lisuride is the most potent stereospecific partial agonist for the human H1R reported to date.
    • The discovery provides a valuable pharmacological tool for in vitro characterization of the H1R.
    • This research opens avenues for exploring therapeutic applications of H1R agonists.