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

5-HT 1B/D receptor antagonists

P J Pauwels1

  • 1Centre de Recherche Pierre Fabre, Laboratory of Cellular and Molecular Neurobiology, Castres, France. CRPF1@STARWAY.TM.FR.PAUWELS

General Pharmacology
|September 1, 1997
PubMed
Summary

Selective 5-HT 1B/D receptor antagonists, like benzanilides, are crucial for modulating serotonin neurotransmission. Future research should focus on developing selective ligands to explore therapeutic potential in neurological disorders.

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

Effect of oxygen and glucose availability on the glycolytic rate in neuroblastoma cells under different conditions of culture.

Neurochemistry international·2010
Same author

Agonist-induced desensitization of 5-HT(2) receptors on cultured calf aortic smooth muscle cells.

Neurochemistry international·2009
Same author

Mutation in a protein kinase C phosphorylation site of the 5-HT1A receptor preferentially attenuates Ca2+ responses to partial as opposed to higher-efficacy 5-HT1A agonists.

Neuropharmacology·2003
Same author

Large-amplitude 5-HT1A receptor activation: a new mechanism of profound, central analgesia.

Neuropharmacology·2002
Same author

Sign-reversal during persistent activation in mu-opioid signal transduction.

Journal of theoretical biology·2002
Same author

Evidence for protean agonism of RX 831003 at alpha 2A-adrenoceptors by co-expression with different G alpha protein subunits.

Neuropharmacology·2002

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • 5-Hydroxytryptamine-1B (5-HT 1B) and 5-hydroxy-tryptamine-1D (5-HT 1D) receptors are key mediators of serotonergic neurotransmission.
  • These G-protein-coupled receptors are found in brain regions like the globus pallidus and substantia nigra.
  • Presynaptic 5-HT 1B/D receptors regulate the release of serotonin and other neurotransmitters, while postsynaptic receptors are implicated in disorders like OCD.

Purpose of the Study:

  • To investigate the efficacy of available 5-HT 1B/D receptor antagonists.
  • To differentiate between neutral antagonists, partial agonists, and inverse agonists at recombinant human 5-HT 1B and 5-HT 1D receptor sites.
  • To evaluate the potential of selective 5-HT 1B/D receptor blockade for therapeutic applications.

Main Methods:

  • Utilized a [35S]-GTP gamma S binding assay on membrane preparations of stably transfected rat C6-glial cell lines.
  • Measured efficacy at recombinant human 5-HT 1B and 5-HT 1D receptor subtypes.
  • Assessed both selective (GR 127935, GR 125743) and nonselective (metergoline, 1-naphthylpiperazine, methiothepin, ketanserin, ritanserin) ligands.

Main Results:

  • Selective ligands GR 127935 and GR 125743 exhibited significant intrinsic activity (43–69%) at the 5-HT 1D receptor, indicating partial agonist properties.
  • Nonselective ligand 1-naphthylpiperazine showed lower intrinsic activity (15–19%) at both subtypes.
  • Methiothepin, ketanserin, and ritanserin acted as inverse agonists, displaying negative efficacy (-14% to -28%) at both receptor subtypes.

Conclusions:

  • Many commonly used 5-HT 1B/D receptor ligands are not neutral antagonists but possess partial agonist or inverse agonist properties.
  • Differential blockade of 5-HT 1B/D receptors by neutral antagonists versus inverse agonists can modulate 5-HT neurotransmission.
  • Future development should focus on identifying selective 5-HT 1B and 5-HT 1D receptor ligands with neutral antagonist or inverse agonist profiles to explore therapeutic potential.

Related Experiment Videos