Uses
A highly selective histamine H4 receptor silent antagonist
Biological Activity
Highly selective histamine H 4 receptor silent antagonist; binds with high affinity to the human H 4 receptor (K i = 26 nM) and is > 540-fold selective over the H 3 receptor (K i = 14.1 μ M). In vitro, inhibits mast cell and eosinophil chemotaxis with IC 50 values of 138 and 530 nM respectively. Orally active in vivo .
in vivo
JNJ10191584 maleate (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice[1].
JNJ10191584 maleate (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice[1].
JNJ10191584 maleate (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice[1].
IC 50
Human H
4 Receptor: 26 nM (Ki); human H
3 receptor: 14.1 μM (Ki)
storage
room temperature (desiccate)
![1-[(5-CHLORO-1H-BENZIMIDAZOL-2-YL)CARBONYL]-4-METHYLPIPERAZINE MALEATE Structure](https://www.chemicalbook.com/CAS/GIF/869497-75-6.gif)
