产品
编 号:F403970
分子式:C23H28Cl2F2N2O3
分子量:489.38
产品类型
结构图
CAS No: 607736-84-5
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产品详情
生物活性:
SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with Ki of 9.7 nM.
体内研究:
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.
体外研究:
SUN-1334H causes potent inhibition of histamine induced contractions of isolated guinea-pig ileum with an IC50 (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.