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. 2010 Mar:59 Suppl 2:S249-51.
doi: 10.1007/s00011-009-0143-2.

Lead identification and optimization of diaminopyrimidines as histamine H4 receptor ligands

K Sander  1 , T Kottke, E Proschak, Y Tanrikulu, E H Schneider, R Seifert, G Schneider, H Stark
Affiliations

Lead identification and optimization of diaminopyrimidines as histamine H4 receptor ligands

K Sander et al. Inflamm Res. 2010 Mar.

Abstract

Background: The human histamine H(4) receptor (hH(4)R) is a promising new target in the therapy of inflammatory or immune system diseases.

Methods: For the development of new hH(4)R ligands, a broad virtual screening was performed and two hits were identified. Their annelated heterocyclic core was optimized with regard to affinity and potency.

Results: Pharmacological characterization of the resulting diaminopyrimidines revealed different agonist and antagonist properties within the same scaffold.

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