SUN 1334H 

SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with K_i of 9.7 nM.

Ki: 9.7 nM (H1 receptor)^[1]

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^[1]. SUN-1334H, cetirizine and hydroxyzine cause comparable inhibition of NLF leukocytes, IL-4 and total protein concentrations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1]. 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

489.38

C₂₃H₂₈Cl₂F₂N₂O₃

607736-84-5

Solid

Light yellow to yellow

O=C(O)COC/C=C/CN1CCN(C(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3)CC1.[H]Cl.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [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.  [Content Brief]

  [2]. Mandhane SN, et al. Characterization of anti-inflammatory properties and evidence for no sedation liability for the novel antihistamine SUN-1334H. Int Arch Allergy Immunol. 2010;151(1):56-69.  [Content Brief]