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Aryl biphenyl-3-ylmethylpiperazines as 5-HT7 Receptor Antagonists

Aryl biphenyl-3-ylmethylpiperazines as 5-HT7 Receptor Antagonists

Jeeyeon Kim, Youngjae Kim, Jinsung Tae, Miyoung Yeom, Bongjin Moon, Xi-Ping Huang, Bryan L Roth, Kangho Lee, Hyewhon Rhim, Il Han Choo, Youhoon Chong, Gyochang Keum, Ghilsoo Nam, Hyunah Choo

ChemMedChem. 2013 Nov;8(11):1855-64.

PMID: 24039134

Abstract:

The 5-HT7 receptor (5-HT7 R) is a promising therapeutic target for the treatment of depression and neuropathic pain. The 5-HT7 R antagonist SB-269970 exhibited antidepressant-like activity, whereas systemic administration of the 5-HT7 R agonist AS-19 significantly inhibited mechanical hypersensitivity and thermal hyperalgesia. In our efforts to discover selective 5-HT7 R antagonists or agonists, aryl biphenyl-3-ylmethylpiperazines were designed, synthesized, and biologically evaluated against the 5-HT7 R. Among the synthesized compounds, 1-([2'-methoxy-(1,1'-biphenyl)-3-yl]methyl)-4-(2-methoxyphenyl)piperazine (28) was the best binder to the 5-HT7 R (pKi =7.83), and its antagonistic property was confirmed by functional assays. The selectivity profile of compound 28 was also recorded for the 5-HT7 R over other serotonin receptor subtypes, such as 5-HT1 R, 5-HT2 R, 5-HT3 R, and 5-HT6 R. In a molecular modeling study, the 2-methoxyphenyl moiety attached to the piperazine ring of compound 28 was proposed to be essential for the antagonistic function.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP16400503	3,3′,5,5′-Tetrabromo-1,1′-biphenyl		16400-50-3	Price

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