AI Article Synopsis
- Three series of H(4) receptor ligands have been created and their effectiveness tested through various assays.
- Modifying small lipophilic groups on specific positions of the compounds improved their activity in competitive binding tests.
- Two compounds, indole 8 and benzimidazole 40, emerged as strong H(4) antagonists and showed promise in further studies related to mast cell and eosinophil movement.
Article Abstract
Three series of H(4) receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H(4) receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [(3)H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H(4) antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.
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