GT 2016
GT 2016 is an antagonist of histamine H3 receptors (Ki = 43.8 nM).{51179} It is selective for H3 over H1 and H2 receptors (IC50 = >10,000 nM for both) and lacks activity against kidney and brain histamine methyltransferase at concentrations up to 3 ?M. In vivo, GT 2016 (10 and 30 mg/kg) increases histamine release in the rat parietal cortex.
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11996-5
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