Effects of EGIS-7625, a Selective and Competitive 5-HT2B Receptor Antagonist

@article{Kovcs2004EffectsOE,
  title={Effects of EGIS-7625, a Selective and Competitive 5-HT2B Receptor Antagonist},
  author={Anik{\'o} Kov{\'a}cs and Istv{\'a}n Gacs{\'a}lyi and Janos Dr. Wellmann and {\'E}va Schmidt and Z Sz{\"u}cs and Val{\'e}rie Dubreuil and Jean Paul Nicolas and Jean A. Boutin and D{\'a}niel B{\'o}zsing and Andr{\'a}s Egyed and K. Tihanyi and Michael Spedding and G{\'a}bor Sz{\'e}n{\'a}si},
  journal={Cardiovascular Drugs and Therapy},
  year={2004},
  volume={17},
  pages={427-434}
}
Our aim was to specify the 5-HT2 subtype selectivity of EGIS-7625 (1-benzyl-4-[(2-nitro-4-methyl-5-amino)-phenyl]-piperazine), a new 5-HT2B ligand, in receptor binding studies and characterize its pharmacology at 5-HT2A, 5-HT2B and 5-HT2C receptors in in vivo experiments and in isolated organs, in vitro. EGIS-7625 had high affinity for recombinant human 5-HT2B receptors (pKi = 9.0) but much weaker affinity for 5-HT2A and 5-HT2C receptors (pKi = 6.2 and 7.7, respectively). In the classic 5-HT2B… 

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