(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE
(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE Basic information
- Product Name:
- (6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE
- Synonyms:
-
- JNJ 10191584
- PIPERAZINE, 1-[(5-CHLORO-1H-BENZIMIDAZOL-2-YL)CARBONYL]-4-METHYL-
- (6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE
- Methanone, (6-chloro-1H-benzimidazol-2-yl)(4-methyl-1-piperazinyl)-
- 6-chloro-2-(4-methylpiperazine-1-carbonyl)-1H-1,3-benzodiazole
- (5-Chloro-1H-benzo[d]imidazol-2-yl)(4-methylpiperazin-1-yl)methanone
- CAS:
- 73903-17-0
- MF:
- C13H15ClN4O
- MW:
- 278.74
- Mol File:
- 73903-17-0.mol
(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE Chemical Properties
- form
- Solid
- color
- White to off-white
(6-CHLORO-1H-BENZOIMIDAZOL-2-YL)-(4-METHYL-PIPERAZIN-1-YL)-METHANONE Usage And Synthesis
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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