Chemical Name: (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
Biological ActivityPotent histamine H4 receptor antagonist (pKi values are 8.24 and 8.47 in human and rat H4 receptors respectively). Displays 162-fold, 620-fold, and > 1600-fold selectivity over human H3, H1 and H2 receptors. Blocks zymosan-induced neutrophil reflux and attenuates thermal hypersensitivity in vivo (ED50 = 42 μmol/kg, ip).
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Molecular and biochemical pharmacology of the histamine H4 receptor.
Leurs et al.
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Liu et al.
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