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. 2011 Jan;336(1):30–37. doi: 10.1124/jpet.110.171264

TABLE 1.

H3R ligands that have been commonly used in pain research

Drug Classification Reference
BP 2–94 H3 agonist prodrug Rouleau et al., 1997
GSK189254 H3 inverse agonista Medhurst et al., 2008
Imetit H3 agonistb Vollinga et al., 1994
Immepip H3 agonistb Vollinga et al., 1994
RAMH H3 agonist Arrang et al., 1987
Thioperamide H3 inverse agonista Arrang et al., 1987
a

Because nearly all H3 antagonists have inverse agonist properties in vitro, the terms “antagonist” and “inverse agonist” are used interchangeably in the present work.

b

Has weaker, but possibly relevant, histamine H4 receptor affinity (Lim et al., 2005).

HHS Vulnerability Disclosure