Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.

@article{Esbenshade2003TwoNA,
  title={Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.},
  author={Timothy A. Esbenshade and Kathleen M. Krueger and Thomas R. Miller and Chae Hee Kang and Lynne I Denny and David G. Witte and Betty Bei Yao and Gerard B. Fox and Ramin Faghih and Youssef L. Bennani and Michael Kevin Williams and Arthur A. Hancock},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2003},
  volume={305 3},
  pages={
          887-96
        }
}
Histamine H3 receptor (H3R) antagonists enhance neurotransmitter release and are being developed for the treatment of a variety of neurological and cognitive disorders. Many potent histamine H3R antagonists contain an imidazole moiety that limits receptor selectivity and the tolerability of this class of compounds. Here we present the in vitro pharmacological data for two novel piperazine amide ligands, A-304121 [4-(3-((2R)-2-aminopropanoyl-1-piperazinyl)propoxy)phenyl)cyclopropylmethanone] and… CONTINUE READING

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