Protein Information

Name interleukin 1beta
Synonyms Catabolin; IL 1; IL 1 beta; IL 1B; IL1 beta; IL1B; IL1F2; Interleukin 1…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
18078749 Lee GE, Joshi BV, Chen W, Jeong LS, Moon HR, Jacobson KA, Kim YC: Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor. Bioorg Med Chem Lett. 2008 Jan 15;18(2):571-5. Epub 2007 Nov 28.

Analogues of the P2X (7) receptor antagonist KN-62, modified at the piperazine and arylsulfonyl groups, were synthesized and assayed at the human P2X (7) receptor for inhibition of BzATP-induced effects, that is, uptake of a fluorescent dye (ethidium bromide) in stably transfected HEK293 cells and IL-1beta release in differentiated THP-1 cells.
31(0,1,1,1) Details
12672232 Baraldi PG, del Carmen Nunez M, Morelli A, Falzoni S, Di Virgilio F, Romagnoli R: Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor. J Med Chem. 2003 Apr 10;46(8):1318-29.

The present study was designed to evaluate the functional antagonistic properties of a novel series of KN-62-related compounds characterized by the presence of different phenyl-substituted piperazine moieties.
The biological responses investigated were ATP-dependent Ca (2+) influx across the plasma membrane, ethidium bromide uptake, and secretion of the cytokine interleukin-1beta.
4(0,0,0,4) Details
18595695 Betschmann P, Bettencourt B, Donnelly-Roberts D, Friedman M, George J, Hirst G, Josephsohn N, Konopacki D, Li B, Maull J, Morytko MJ, Moore NS, Namovic M, Rafferty P, Salmeron-Garcia JA, Tarcsa E, Wang L, Woller K: Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists. . Bioorg Med Chem Lett. 2008 Jul 15;18(14):3848-51. Epub 2008 Jun 20.

Compounds were assayed for activity at human and rat P2X (7) receptors in addition to their ability to inhibit IL-1 beta release from stimulated human whole blood cultures.
1(0,0,0,1) Details
15665918 Nikitin AA, Abidov MT, Kovalevskaya EO, Kalyuzhin OV: Search for potent modulators of cytokine production by macrophages. . Bull Exp Biol Med. 2004 Sep;138(3):259-61.


We compared the effects of Tamerit, Polyoxidony, and Licopid on spontaneous and lipopolysaccharide-stimulated production of interleukin-1 and tumor necrosis factor by mouse peritoneal macrophages in vitro.
1(0,0,0,1) Details
18771755 Hwang J, Zheng LT, Ock J, Lee MG, Suk K: Anti-inflammatory effects of m-chlorophenylpiperazine in brain glia cells. Int Immunopharmacol. 2008 Dec 10;8(12):1686-94. Epub 2008 Sep 2.


Our results showed that m-CPP significantly decreased the production of nitric oxide, tumor necrosis factor-alpha (TNF-alpha), and interleukin-1beta (IL-1beta) in microglia and astrocyte cultures. m-CPP also attenuated the expression of inducible nitric oxide synthase and pro-inflammatory cytokines such as IL-1beta and TNF-alpha at mRNA levels.
1(0,0,0,1) Details
17328048 Kelso EB, Ferrell WR, Lockhart JC, Elias-Jones I, Hembrough T, Dunning L, Gracie JA, McInnes IB: Expression and proinflammatory role of proteinase-activated receptor 2 in rheumatoid synovium: ex vivo studies using a novel proteinase-activated receptor 2 antagonist. Arthritis Rheum. 2007 Mar;56(3):765-71.


Importantly, spontaneous release of tumor necrosis factor alpha and interleukin-1beta from RA synovium was substantially inhibited by ENMD-1068, in a dose-dependent manner.
1(0,0,0,1) Details
15454114 Dyakonova VA, Dambaeva SV, Pinegin BV, Khaitov RM: Study of interaction between the polyoxidonium immunomodulator and the human immune system cells. Int Immunopharmacol. 2004 Dec 15;4(13):1615-23.

Polyoxidonium (PO) is a high-molecular weight physiologically active compound with pronounced immunomodulating activity, an N-oxidized polyethylene-piperazine derivative.
The analysis of immunomodulating effect produced by PO proved its stimulating activity on some cytokines production in vitro, e.g. interleukin 1beta (IL-1beta), tumor necrosis factor (TNF)-alpha and IL-6.
1(0,0,0,1) Details