Proxyfan
Proxyfan is a histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist, to antagonist, to inverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 receptor. This gives it a complex activity profile in vivo which has proven useful for scientific research.
References
↑ Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM. High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature. 2000 Dec 14;408(6814):860-4. PMID 11130725
↑ Fox GB, Pan JB, Esbenshade TA, Bitner RS, Nikkel AL, Miller T, Kang CH, Bennani YL, Black LA, Faghih R, Hancock AA, Decker MW. Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model. Pharmacology, Biochemistry and Behaviour. 2002 Jun;72(3):741-50. PMID 12175472
↑ Gbahou F, Rouleau A, Morisset S, Parmentier R, Crochet S, Lin JS, Ligneau X, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM. Protean agonism at histamine H3 receptors in vitro and in vivo. Proceedings of the National Academy of Sciences USA. 2003 Sep 16;100(19):11086-91. PMID 12960366
