607736-84-5

Ki: 9.7 nM (H1 receptor)

SUN-1334H causes potent inhibition of histamine induced contractions of isolated guinea-pig ileum with an IC ₅₀ (half the maximal inhibitory concentration) of 0.198 μM. In CHO-K1/hERG cells, SUN-1334H does not modulate hERG K ⁺ -currents at concentrations as high as 100 μM. SUN-1334H, cetirizine and hydroxyzine cause comparable inhibition of NLF leukocytes, IL-4 and total protein concentrations.

SUN-1334H potently inhibits histamine-induced bronchospasm over 24 hours following oral administration and completely suppresses histamine-induced skin wheal in beagle dogs and ovalbumin-induced rhinitis in guinea pigs. In skin allergy models, SUN-1334H shows potent reduction of passive and active cutaneous anaphylactic reactions. In central nervous system side effects models, SUN-1334H, desloratadine and fexofenadine are devoid of any significant effects.