Protein Information

Name histamine H3 receptors
Synonyms G protein coupled receptor 97; GPCR97; HH3R; HRH 3; HRH3; Histamine H3 receptor; Histamine receptor H3; Histamine H3 receptors…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
12755406 Faghih R, Phelan K, Esbenshade TA, Miller TR, Kang CH, Krueger KM, Yao BB, Fox GB, Bennani YL, Hancock AA: D-alanine piperazine-amides: novel non-imidazole antagonists of the histamine H3 receptor. Inflamm Res. 2003 Apr;52 Suppl 1:S47-8.
81(1,1,1,1) Details
15642406 Walczynski K, Zuiderveld OP, Timmerman H: Non-imidazole histamine H3 ligands. Eur J Med Chem. 2005 Jan;40(1):15-23.

In search for a new lead of non-imidazole histamine H3-receptor antagonists, a series of 1 [(2-thiazolopyridine)-4-n-propyl] piperazines, the analogous 1-[(2-oxazolopyridine)-4-npropyl] piperazines, 1-[(2-benzothiazole)-4-n-propyl] piperazine and 1-[(2-benzooxazole) 4-n-propyl] piperazine were prepared and in vitro tested as H3-receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum).
31(0,1,1,1) Details
12606603 Esbenshade TA, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Fox GB, Faghih R, Bennani YL, Williams M, Hancock AA: Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96. Epub 2003 Feb 20.

Here we present the in vitro pharmacological data for two novel piperazine amide ligands, A-304121 [4-(3-((2R)-2-aminopropanoyl-1-piperazinyl) propoxy) phenyl) cyclopropylmetha none] and A-317920 [N-((1R)-2-(4-(3-(4-(cyclopropylcarbonyl) phenoxy) propyl)-1-piperazinyl)-1- methyl-2-oxo-ethyl-)-2-furamide], and compare them with the imidazole H3R antagonists ciproxifan, clobenpropit, and thioperamide.
2(0,0,0,2) Details
12606600 Fox GB, Pan JB, Radek RJ, Lewis AM, Bitner RS, Esbenshade TA, Faghih R, Bennani YL, Williams M, Yao BB, Decker MW, Hancock AA: Two novel and selective nonimidazole H3 receptor antagonists A-304121 and A-317920: II. J Pharmacol Exp Ther. 2003 Jun;305(3):897-908. Epub 2003 Feb 20.

A-304121 and A-317920 represent a series of novel, H3R-selective piperazine amides that enhance cognition in vivo, which could offer advantages over existing H3R antagonists or cognition-enhancing agents.
Pharmacological blockade of central histamine H3 receptors (H3Rs) enhances cognition in rodents and offers promise for the clinical treatment of neurological disorders.
1(0,0,0,1) Details