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Proxyfan Oxalate is a potent histamine H3 receptor antagonist with Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors[1][2]. | [IC 50]
Rat H3LR: 2.9 nM (Ki); Human H3LR: 2.7 nM (Ki) | [References]
[1] X Ligneau, et al. Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol. 2000 Dec;131(7):1247-50. DOI:10.1038/sj.bjp.0703712
[2] R H Clapp, et al. Proxyfan acts as a neutral antagonist of histamine H3 receptors in the feeding-related hypothalamic ventromedial nucleus. Br J Pharmacol. 2012 Nov;167(5):1099-110. DOI:10.1111/j.1476-5381.2012.02056.x |
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