• Corpus ID: 26524521

Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.

@article{Yates1999IdentificationAP,
  title={Identification and pharmacological characterization of a series of new 1H-4-substituted-imidazoyl histamine H3 receptor ligands.},
  author={Stephen L. Yates and James G. Phillips and Rosilyn Gregory and Gary Pawlowski and Leena Fadnis and M. A. Khan and S. Mubarik Ali and Clark E. Tedford},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1999},
  volume={289 2},
  pages={
          1151-9
        }
}
A new series of 1H-4-substituted imidazole compounds were synthesized and identified as potent and selective histamine (HA) H3 receptor ligands. These ligands establish that HA H3 antagonists exhibit stereoselective and conformational preferences in their binding to the HA H3 receptor. Structure-activity relationships were determined in vitro by HA H3 receptor-binding affinities using [3H]Nalpha-methylhistamine and rat cerebral cortical tissue homogenates. Several derivatives containing olefin… 

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The present studies extend the structure-activity relationships for optimal HA H3 receptor affinity and central nervous system penetration by incorporation of a conformationally restricted cyclopropane nucleus by extending the understanding of ligand-receptor interactions at the HA H1 receptor with the development of high affinity HA H2 receptor antagonists containing a stereochemical presentation.
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