Table 4.
H3 Receptor Antagonists
| Receptor | H3 |
|---|---|
| Signal conduction through | Gi/o |
| Location of receptors | Mainly expressed on presynaptic nerves in the peripheral sympathetic adrenergic system and histaminergic nerves in the central nervous system. Receptors can be found in airways and gastrointestinal tract |
| Chromosome location | 20q13.33 |
| Signal conduction induces | Decreased cyclic AMP, induction MAP kinase |
| Antagonists (reverse agonists) | None available clinically: Thioperamide, alobenpropit, and others Very little data regarding effect of H1 antagonists on the H3 receptor are available (13) |
| Activities | Opposes bronchoconstriction and gastric acid; suppression of norepinephrine release at presynaptic nerve endings |
| Nasal symptoms produced | Can produce nasal decongestion by blocking effect of histamine on adrenergic postsynaptic receptors |