607737-00-8

SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs[1].

H₁ Receptor: 20.3 nM (IC₅₀); Dopamine D3 receptor: 3.43 μM (IC₅₀); σ1: 5.46 μM (IC₅₀); Alpha-1D adrenergic receptor: 7.76 μM (IC₅₀)

[1] Mandhane SN, et al., Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112. DOI:10.2165/00126839-200809020-00004