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 |
Because nearly all H3 antagonists have inverse agonist properties in vitro, the terms “antagonist” and “inverse agonist” are used interchangeably in the present work.
Has weaker, but possibly relevant, histamine H4 receptor affinity (Lim et al., 2005).