SUN 1334H

Names

[ CAS No. ]:
607736-84-5

[ Name ]:
SUN 1334H

[Synonym ]:
{[(2E)-4-{4-[Bis(4-fluorophenyl)methyl]-1-piperazinyl}-2-buten-1-yl]oxy}acetic acid dihydrochloride
Acetic acid, 2-[[(2E)-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-2-buten-1-yl]oxy]-, hydrochloride (1:2)

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Research Areas >> Inflammation/Immunology

[Target]

Ki: 9.7 nM (H1 receptor)[1]


[In Vitro]

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].

[In Vivo]

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].

[References]

[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.

[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.


[Related Small Molecules]

Loratadine | Histamine | Pitolisant hydrochloride | Cimetidine | Osthole | Clemastine fumarate | Ebrotidine | JNJ-7777120 | Famotidine | Cetirizine Dihydrochloride | Desloratadine | Ketotifen fumarate | Lodoxamide | Meclizine dihydrochloride | Chlorpheniramine maleate

Chemical & Physical Properties

[ Molecular Formula ]:
C23H28Cl2F2N2O3

[ Molecular Weight ]:
489.383

[ Exact Mass ]:
488.144501

[ Storage condition ]:
2-8℃

Related Compounds