Inverse Agonists and Serotonergic Transmission: From Recombinant, Human Serotonin (5-HT)1B Receptors to G-Protein Coupling and Function in Corticolimbic Structures in vivo

@article{Millan1999InverseAA,
  title={Inverse Agonists and Serotonergic Transmission: From Recombinant, Human Serotonin (5-HT)1B Receptors to G-Protein Coupling and Function in Corticolimbic Structures in vivo},
  author={M. J. Millan and Alain P Gobert and Val{\'e}rie Audinot and Anne Dekeyne and Adrian Newman-Tancredi},
  journal={Neuropsychopharmacology},
  year={1999},
  volume={21},
  pages={61S-67S}
}
The concept of inverse agonism, whereby “antagonists” exert actions opposite to those of agonists at constitutively active receptors, has been documented both at receptor-modulated ion channels as well as at G-protein-coupled receptors (GPCR) in recombinant expression systems. However, it remains unclear whether physiologically or therapeutically relevant inverse agonists actions at GPCRs occur in the CNS in vivo. The present overview discusses our recent observations concerning 5-HT1B… CONTINUE READING
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S18127: A novel and selective, aminopiperidine antagonist at serotonin (5-HT)1B/1D receptors

  • MJ Millan, V Audinot, +6 authors J-L Peglion
  • Am Soc Neurosci
  • 1998
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