Pharmacological Properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological Characterization and Broad Preclinical Efficacy in Cognition and Schizophrenia of a Potent and Selective Histamine H3 Receptor Antagonist

@article{Fox2005PharmacologicalPO,
  title={Pharmacological Properties of ABT-239 [4-(2-\{2-[(2R)-2-Methylpyrrolidinyl]ethyl\}-benzofuran-5-yl)benzonitrile]: II. Neurophysiological Characterization and Broad Preclinical Efficacy in Cognition and Schizophrenia of a Potent and Selective Histamine H3 Receptor Antagonist},
  author={G. Fox and T. Esbenshade and J. B. Pan and R. Radek and K. Krueger and B. Yao and K. Browman and M. J. Buckley and M. E. Ballard and V. Komater and H. Miner and Min Zhang and R. Faghih and L. Rueter and R. Bitner and K. Drescher and J. Wetter and K. Marsh and M. Lemaire and R. Porsolt and Y. Bennani and J. Sullivan and M. Cowart and M. Decker and A. Hancock},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2005},
  volume={313},
  pages={176 - 190}
}
  • G. Fox, T. Esbenshade, +22 authors A. Hancock
  • Published 2005
  • Chemistry, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
  • Acute pharmacological blockade of central histamine H3 receptors (H3Rs) enhances arousal/attention in rodents. However, there is little information available for other behavioral domains or for repeated administration using selective compounds. ABT-239 [4-(2-{2-[(2R)-2-methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile] exemplifies such a selective, nonimidazole H3R antagonist with high affinity for rat (pKi = 8.9) and human (pKi = 9.5) H3Rs. Acute functional blockade of central H3 Rs was… CONTINUE READING
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