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

Selective and functional 5-hydroxytryptamine4 receptor antagonism by SB 207266

K A Wardle1, S Bingham, E S Ellis

  • 1SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex.

British Journal of Pharmacology
|June 1, 1996
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

Neural networks involved in nausea in adult humans: A systematic review.

Autonomic neuroscience : basic & clinical·2022
Same author

Studying the aging of Laponite suspensions using extensional rheology.

The European physical journal. E, Soft matter·2022
Same author

Topographic Control of Order in Quasi-2D Granular Phase Transitions.

Physical review letters·2022
Same author

Slip in adhesion tests of a Kaolin clay.

The European physical journal. E, Soft matter·2021
Same author

Collision-enhanced friction of a bouncing ball on a rough vibrating surface.

Scientific reports·2021
Same author

Farnesoid X receptor - a molecular predictor of weight loss after vertical sleeve gastrectomy?

Obesity science & practice·2019

SB 207266 is a potent and selective 5-HT4 receptor antagonist, demonstrating efficacy in both in vitro and in vivo models. This novel orally active amide offers a valuable tool for studying 5-HT4 receptor function.

Area of Science:

  • Pharmacology
  • Gastroenterology
  • Neuroscience

Background:

  • The 5-HT4 receptor plays a role in gastrointestinal motility and other physiological processes.
  • Selective antagonists are crucial for understanding receptor function and developing therapeutics.

Purpose of the Study:

  • To characterize the pharmacological profile of SB 207266, a novel 5-HT4 receptor antagonist.
  • To evaluate its potency, selectivity, and activity in vitro and in vivo.

Main Methods:

  • In vitro studies using guinea-pig distal colon longitudinal muscle myenteric plexus (LMMP) to assess 5-HT-evoked contractions.
  • In vivo studies in the dog Heidenhain pouch model to evaluate antagonism of 5-HT-evoked contractions after oral and intravenous administration.

Main Results:

Related Experiment Videos

  • SB 207266 demonstrated high potency (apparent pA2 10.6 +/- 0.1) and selectivity as a 5-HT4 receptor antagonist in guinea-pig colon.
  • In dogs, SB 207266 dose-dependently antagonized 5-HT-evoked contractions with ID50 values of 1.3 µg/kg (i.v.) and 9.6 µg/kg (oral).
  • Antagonistic effects were reversible and long-lasting, particularly after oral administration.

Conclusions:

  • SB 207266 is a highly potent, selective, and orally active 5-HT4 receptor antagonist.
  • It represents the first orally active amide antagonist in this class.
  • SB 207266 is a significant new tool for in vitro and in vivo research on 5-HT4 receptor function.