High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models.

@article{Tedford1998HighAP,
  title={High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models.},
  author={Clark E. Tedford and Marcel Hoffmann and Nahid Seyedi and Ryushi Maruyama and Roberto Levi and Stephen L. Yates and S. Mubarik Ali and James G. Phillips},
  journal={European journal of pharmacology},
  year={1998},
  volume={351 3},
  pages={
          307-11
        }
}
Two Novel and Selective Nonimidazole Histamine H3 Receptor Antagonists A-304121 and A-317920: I. In Vitro Pharmacological Effects
TLDR
In vitro pharmacological data for two novel piperazine amide ligands represent useful leads for the development of H3R antagonist therapeutic agents.
Pharmacological Properties and Procognitive Effects of ABT-288, a Potent and Selective Histamine H3 Receptor Antagonist
TLDR
ABT-288 is a selective H3R antagonist with broad procognitive efficacy in rodents and excellent drug-like properties that support its advancement to the clinical area.
Pharmacological Properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and Selective Histamine H3 Receptor Antagonist with Drug-Like Properties
TLDR
ABT-239 demonstrates good pharmacokinetic characteristics in rat, dog, and monkey with t1/2 values corresponding with clearance values and metabolic turnover in liver microsomes from these species, and good oral bioavailability ranging from 52 to 89%.
G Protein-Dependent Pharmacology of Histamine H3 Receptor Ligands: Evidence for Heterogeneous Active State Receptor Conformations
TLDR
The results demonstrate that GT-2331 and proxyfan's differential pharmacology at the H3 receptor depends on the type of G protein used and provide indirect evidence for differential ligand-bound active states that mediate signaling by the H2 receptor.
Development of trans-2-[1H-imidazol-4-yl] cyclopropane derivatives as new high-affinity histamine H3 receptor ligands.
TLDR
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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