| Name | G protein coupled receptors |
|---|---|
| Synonyms | ASRT 2; ASRT2; G protein coupled receptor 154; G protein coupled receptor for asthma susceptibility; G protein coupled receptor; G protein coupled receptor PGR14; GPR154; GPRA… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| 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. |
31(0,1,1,1) | 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 mobilization and increases in cAMP levels. |
6(0,0,0,6) | Details |
| 12769714 | Boyle CD, Palani A: Structure-activity relationship studies: M2 and CCR5 receptor antagonists. . Curr Top Med Chem. 2003;3(10):1155-69. The most familiar G-protein-coupled receptors are muscarinic receptors, adrenergic receptors, dopaminergic receptors and opioid receptors. |
3(0,0,0,3) | Details |
| 19605522 | Cussac D, Palmier C, Finana F, De Vries L, Tardif S, Leger C, Bernois S, Heusler P: Mutant 5-hydroxytryptamine 1A receptor D116A is a receptor activated solely by synthetic ligands with a rich pharmacology. J Pharmacol Exp Ther. 2009 Oct;331(1):222-33. Epub 2009 Jul 15. Like other biogenic amine G protein-coupled receptors, mutation of the conserved aspartatic residue into at position 116 (D116A (3.32)) in the (5-HT)(1A) receptor greatly affects binding and signal transduction. [(3) H] 8-Hydroxy-2-dipropylaminotetralin (8-OH-DPAT) and [(3) H]-N-(2-(4-(2-methoxyphenyl)-1-piperazinyl) ethyl)-N-(2-pyridinyl) cyclo hexanecarboxamide trihydrochloride (WAY100,635) are capable to bind the 5-HT (1A)-D116A mutant and, using these radioligands, we show here that this mutation dramatically reduces the affinities of the selective 5-HT (1A) agonists N-(3-chloro-4-fluorobenzoyl)-4--4-[(5-methylpyridin-2-yl)-methylamin o methyl] piperidine (F13640), 3-chloro-4-fluorophenyl-(4-fluorophenyl-4-{[(5-methyl-6 methylamino-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone (F13714), and 2-[5-[3-(4-methylsulfonylamino) benzyl-1,4-oxadiazol-5-yl]-1H-indole-3-yl] e thylamine (L694247) and that of 5-carboxamidotryptamine. In contrast, affinities of the 5-HT (1A) ligands WAY100,635, spiperone, (-)-4-(dipropylamino)-1,3,4,5-tetrahydrobenz {c,d}indole-6-carboxamide (LY228,729), and 1-[2-(4-fluorobenzoylamino) ethyl]-4-(7-methoxynaphtyl) piperazine (S14506) and the prototypical 5-HT (1A) agonist (+)-8-OH-DPAT are only slightly affected by the mutation, suggesting a moderate contribution of Asp116 to the binding pocket for these latter. |
1(0,0,0,1) | 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. Agonist-induced internalization of G protein-coupled receptors (GPCRs) is a well characterized phenomenon believed to contribute to receptor desensitization. In this study, we have examined the effects of 5-HT2C receptor agonists 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 |
| 11100975 | Harikumar KG, John PT, Chattopadhyay A: Role of disulfides and sulfhydryl groups in agonist and antagonist binding in serotonin1A receptors from bovine hippocampus. Cell Mol Neurobiol. 2000 Dec;20(6):665-81. Since disulfide bonds and sulfhydryl groups have been shown to play vital roles in the assembly, organization, and function of various G-protein-coupled receptors, we report here the effect of disulfide and sulfhydryl group modifications on the agonist and antagonist binding activity of 5-HT1A receptors from bovine hippocampus. 2. |
1(0,0,0,1) | Details |
| 16005846 | Pucadyil TJ, Chattopadhyay A: modulates the antagonist-binding function of hippocampal serotonin1A receptors. Biochim Biophys Acta. 2005 Aug 1;1714(1):35-42. Since a significant portion of the protein lies embedded in the membrane and the ligand-binding pocket is defined by the transmembrane stretches in such receptors, membrane composition and organization represent a crucial parameter in the structure-function analysis of G-protein coupled receptors. |
1(0,0,0,1) | Details |
| 11166326 | Milligan G, Kellett E, Dacquet C, Dubreuil V, Jacoby E, Millan MJ, Lavielle G, Spedding M: S 14506: novel receptor coupling at 5-HT (1A) receptors. . Neuropharmacology. 2001 Mar;40(3):334-44. Thus it is possible to synthesise ligands at G-protein-coupled receptors which are highly potent agonists, but which are structurally related to inverse agonists and show some features of antagonist/inverse agonist binding. |
1(0,0,0,1) | Details |
| 15628665 | Kalipatnapu S, Pucadyil TJ, Harikumar KG, Chattopadhyay A: Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep. 2004 Apr;24(2):101-15. The serotonin1A (5-HT1A) receptors are important members of the superfamily of seven transmembrane domain G-protein coupled receptors. |
1(0,0,0,1) | Details |
| 15595840 | Pucadyil TJ, Kalipatnapu S, Harikumar KG, Rangaraj N, Karnik SS, Chattopadhyay A: G-protein-dependent cell surface dynamics of the human serotonin1A receptor tagged to yellow fluorescent protein. Biochemistry. 2004 Dec 21;43(50):15852-62. The serotonin (1A) receptor is an important member of the superfamily of seven transmembrane domain G-protein-coupled receptors and is the most extensively studied among the serotonin receptors. |
1(0,0,0,1) | Details |
| 15819386 | Sukalovic V, Zlatovic M, Andric D, Roglic G, Kostic-Rajacic S, Soskic V: Interaction of arylpiperazines with the dopamine receptor D2 binding site. Arzneimittelforschung. 2005;55(3):145-52. 178 (VI.44), Trp 182 (VI.48) and Tyr 216 (VII.58) can be considered as a part of the ancillary DAR D2 pocket preserved in most G protein-coupled receptors of the A class and obviously, the arylpiperazine structural motif represents one of the privileged structures that bind to this pocket. The results demonstrated that the interaction of protonated N1 of the piperazine ring with Asp 86 (III.32) and edge-to-face interactions of the aromatic ring of the arylpiperazine part of the ligand with 178 (VI.44), Trp 182 (VI.48) and Tyr 216 (VII.58) of the receptor, represent the major stabilizing forces. |
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. OBJECTIVE: Serine proteinases activate the G protein-coupled receptor, proteinase-activated receptor 2 (PAR-2), via cleavage and exposure of a tethered ligand. |
1(0,0,0,1) | Details |
| 18845198 | Stepanov V, Jarv J: Kinetic mechanism of dopamine transporter interaction with 1-(2-(bis-(4-fluorophenyl) methoxy) ethyl)-4-(3-phenylpropyl) piperazine (GBR 12909). Neurochem Int. 2008 Dec;53(6-8):370-3. Epub 2008 Sep 18. |
0(0,0,0,0) | Details |