Distinctive in vitro signal transduction profile of NLX‐112, a potent and efficacious serotonin 5‐HT1A receptor agonist

@article{NewmanTancredi2017DistinctiveIV,
  title={Distinctive in vitro signal transduction profile of NLX‐112, a potent and efficacious serotonin 5‐HT1A receptor agonist},
  author={Adrian Newman-Tancredi and Jean Claude Martel and Cristina Cosi and Peter Heusler and Fabrice Lestienne and Mark A. Varney and Didier Cussac},
  journal={Journal of Pharmacy and Pharmacology},
  year={2017},
  volume={69}
}
NLX‐112 (befiradol, F13640) is a selective serotonin 5‐HT1A receptor agonist. Although it has been tested in vivo, little has been reported on its in vitro signal transduction profile. 

The selective 5-HT1A receptor agonist NLX-112 displays anxiolytic-like activity in mice

NLX-112 may possess anxiolytic properties which complement its known activity in models of movement disorders, and befiradol, a highly selective, potent and efficacious 5-HT1A receptor full agonist, may be associated with anxiety-like behaviours in mice.

From Receptor Selectivity to Functional Selectivity: The Rise of Biased Agonism in 5-HT1A Receptor Drug Discovery.

The results suggest that opportunities exist for innovative drug discovery of selective 5-HT1A receptor biased agonists that may open new avenues for the treatment of CNS disorders involving dysfunction of serotonergic neurotransmission.

In vivo biased agonism at 5-HT1A receptors: characterisation by simultaneous PET/MR imaging

Combined PET/fMRI represents a powerful tool in neuropharmacology, and opens new ways to address the concept of biased agonism by translational approaches, and demonstrates differential signalling by two 5-HT1A-biased agonists.

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