Identification | Back Directory | [Name]
(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE | [CAS]
73903-17-0 | [Synonyms]
JNJ 10191584 PIPERAZINE, 1-[(5-CHLORO-1H-BENZIMIDAZOL-2-YL)CARBONYL]-4-METHYL- Methanone, (6-chloro-1H-benzimidazol-2-yl)(4-methyl-1-piperazinyl)- (6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE | [Molecular Formula]
C13H15ClN4O | [MDL Number]
MFCD10565946 | [MOL File]
73903-17-0.mol | [Molecular Weight]
278.74 |
Hazard Information | Back Directory | [Uses]
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]. | [Definition]
ChEBI: (6-chloro-1H-benzimidazol-2-yl)-(4-methyl-1-piperazinyl)methanone is a member of benzimidazoles. | [in vivo]
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]. | [IC 50]
Human H4 Receptor: 26 nM (Ki); human H3 receptor: 14.1 μM (Ki) | [References]
[1] Venable JD, et al. Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem. 2005 Dec 29;48(26):8289-98. DOI:10.1021/jm0502081 [2] Sanna MD, et al. Histamine H4 receptor stimulation in the locus coeruleus attenuates neuropathic pain by promoting the coeruleospinal noradrenergic inhibitory pathway. Eur J Pharmacol. 2020 Feb 5;868:172859. DOI:10.1016/j.ejphar.2019.172859 |
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