(R)-(-)-ALPHA-METHYLHISTAMINE DIHYDROBROMIDE

Chemical Properties

White to off-white solid

Uses

R(-)-alpha-Methylhistamine is a potent agonist of the histamine H3-receptor.

Definition

ChEBI: An aralkylamino compound that is histamine bearing a methyl substituent at the alpha-position (the R-enantiomer).

Biological Activity

Very potent, high affinity H 3?agonist (K D = 50.3 nM) that displays > 200-fold selectivity over H 4 receptors. Inhibits H 3 -mediated histamine synthesis and release in the CNS and stimulates H 4 -mediated eosinophil shape change (EC 50 = 66 nM). Also available as part of the Histamine H 3 Receptor Tocriset™ .