Protein Information

Name GPCR
Synonyms GPCR; Putative G protein coupled receptor

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
20213245 Finlay TM, Jayanth P, Amith SR, Gilmour A, Guzzo C, Gee K, Beyaert R, Szewczuk MR: Thymoquinone from nutraceutical black cumin oil activates Neu4 sialidase in live macrophage, dendritic, and normal and type I sialidosis human fibroblast cells via GPCR Galphai proteins and matrix metalloproteinase-9. Glycoconj J. 2010 Apr;27(3):329-48. Epub 2010 Mar 6.

Pertussis toxin (PTX), a specific inhibitor of Galphai proteins of G-protein coupled receptor (GPCR) and the broad range inhibitors of matrix metalloproteinase (MMP) galardin and piperazine applied to live BMC-2, THP-1 and primary BM macrophage cells completely block TQ-induced sialidase activity.
83(1,1,1,3) Details
15113845 Schlag BD, Lou Z, Fennell M, Dunlop J: Ligand dependency of 5-hydroxytryptamine 2C receptor internalization. J Pharmacol Exp Ther. 2004 Sep;310(3):865-70. Epub 2004 Apr 27.

The 5-hydroxytryptamine (5-HT) 2C subtype of serotonin receptor is a GPCR that we have shown to internalize upon agonist incubation.
In this study, we have examined the effects of 5-HT2C receptor agonists serotonin, Ro 60-0175 [(S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine], and WAY-161503 [(4aR)-8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino [1,2-a] quinoxalin-5 (6H) -one]; partial agonists mCPP [1-(m-chlorophenyl) piperazine] and DOI [(+)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane]; inverse agonists SB-206553 [N-3-pyridinyl-3,5-dihydro-5-methylbenzo (1,2-b:4,5-b') dipyrrole-1 (2H) carbo xamide] and mianserin; and neutral antagonists SB-242084 [6-chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-in doline] and 5-methoxygramine on the internalization of a C-terminal green fluorescent protein (GFP)-tagged 5-HT2C receptor (VSV isoform) expressed in transiently transfected human embryonic kidney cells.
1(0,0,0,1) Details
19824051 Guerrini R, Salvadori S, Rizzi A, Regoli D, Calo' G: Neurobiology, pharmacology, and medicinal chemistry of neuropeptide S and its receptor. Med Res Rev. 2009 Oct 12.

Finally, the pharmacological features of substituted bicyclic piperazine molecules (e.g.
NPS selectively binds and activates a previous orphan GPCR, now named NPSR, producing intracellular calcium mobilization and increases in cAMP levels.
1(0,0,0,1) Details