(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE

JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Human H4 Receptor:26 nM (Ki)

human H3 receptor:14.1 μM (Ki)

JNJ10191584 shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively[1]. JNJ10191584 (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1].

JNJ10191584 (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice[1]. JNJ10191584 (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice[1]. JNJ10191584 (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice[1].