| Name | G protein |
|---|---|
| Synonyms | G gamma I; Guanine nucleotide binding protein 2; G protein; GNG 2; GNG2; GNGT 2; GNGT2; Guanine nucleotide binding protein gamma 2… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19043296 | Satoh K, Nonaka R: [In-vitro screening of psychoactive drugs to prevent abuses] . Yakugaku Zasshi. 2008 Dec;128(12):1771-82. These assays were then applied to study the effects of different kinds derivatives, derivatives, and piperazine derivatives) of non-medically used psychoactive drugs on monoamine re-uptake and release, and G-protein binding. |
82(1,1,1,2) | 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. The serotonin1A receptor is the most extensively studied member of the family of seven transmembrane domain G-protein coupled serotonin receptors. |
3(0,0,0,3) | 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. |
3(0,0,0,3) | Details |
| 11860184 | Harikumar KG, Chattopadhyay A: Modulation of antagonist binding to serotonin1A receptors from bovine hippocampus by metal ions. Cell Mol Neurobiol. 2001 Oct;21(5):453-64. The serotonin1A (5-HT1A) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. |
3(0,0,0,3) | Details |
| 11489454 | Jeong HJ, Han SH, Min BI, Cho YW: 5-HT1A receptor-mediated activation of G-protein-gated inwardly rectifying K+ current in rat periaqueductal gray neurons. Neuropharmacology. 2001 Aug;41(2):175-85. I5-HT was mimicked by a 5-HT1A receptor selective agonist, 8-OH-DPAT, and was reversibly blocked by a 5-HT1A receptor antagonist, piperazine but not by a 5-HT2 receptor antagonist, ketanserin. |
2(0,0,0,2) | Details |
| 18367171 | Lee JJ, Hahm ET, Lee CH, Cho YW: 5-HT1A receptor-mediated activation of a G-protein-coupled inwardly rectifying K+ current in rat medial preoptic area neurons. Eur J Pharmacol. 2008 May 31;586(1-3):114-22. Epub 2008 Mar 4. The -activated K+ current was mimicked by a 5-HT1A receptor agonist, (+/-)-8--2-dipropylaminotetralin hydrobromide, and was reversibly blocked by a 5-HT1A receptor antagonist, 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide, but not by a 5-HT2 receptor antagonist, ketanserin. |
2(0,0,0,2) | Details |
| 11068021 | Kishimoto K, Koyama S, Akaike N: Presynaptic modulation of synaptic transmission by tandospirone in rat basolateral amygdala. Eur J Pharmacol. 2000 Nov 3;407(3):257-65. The similar inhibition of miniature IPSC frequency was mimicked by a specific 5-HT1A receptor agonist 8--2-(di-n-propylamino) tetralin (8-OH-DPAT, 1 microM), and the effects of tandospirone were prevented in the presence of a specific 5-HT1A receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190, 1 microM). Furthermore, this presynaptic inhibition by tandospirone was prevented after treatment with a pertussis toxin-sensitive GTP-binding protein (G-protein) inhibitor, N-ethylmaleimide (at 3 microM for 5 min). |
2(0,0,0,2) | Details |
| 16554049 | Cosi C, Carilla-Durand E, Assie MB, Ormiere AM, Maraval M, Leduc N, Newman-Tancredi A: Partial agonist properties of the antipsychotics SSR181507, and bifeprunox at dopamine D2 receptors: G protein activation and prolactin release. Eur J Pharmacol. 2006 Mar 27;535(1-3):135-44. Epub 2006 Mar 22. We compared the effects of the new antipsychotic agents SSR181507 ((3-exo)-8-benzoyl-N-[[(2 s) 7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl] methyl]-8-azabicyclo [3.2.1] oct ane-3- monohydrochloride), bifeprunox (DU127090: 1-(2-Oxo-benzoxazolin-7-yl)-4-(3-biphenyl) methylpiperazinemesylate) and SLV313 (1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4-[5-(4-fluorophenyl)-pyridin-3-ylm ethyl]-piperazine) with those of (7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]-butyloxy)-3,4-dihydro-2 (1 H)-quinolinone), clozapine and haloperidol, on functional measures of dopamine D2 receptor activity in vitro and in vivo: [35S]-GTPgammaS binding to membranes from Sf9 insect cells expressing human D2 Long (hD2 L) receptors, and serum prolactin levels in the rat. |
2(0,0,0,2) | Details |
| 12181435 | Newman-Tancredi A, Cussac D, Marini L, Millan MJ: Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT (1A) receptor-mediated Galpha (i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling. Mol Pharmacol. 2002 Sep;62(3):590-601. Although 5-HT (1A) receptors couple to several Gi/o G-protein subtypes, little is known concerning their differential activation patterns. In contrast, the partial agonists (-)-pindolol and 4-(benzodioxan-5-yl) 1-(indan-2-yl) piperazine (S15535) displayed sigmoidal stimulation isotherms, whereas spiperone and other inverse agonists sigmoidally inhibited [(35) S] GTPgammaS binding. |
2(0,0,0,2) | 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. The serotonin1A (5-HT1A) receptors are members of a superfamily of seven-transmembrane-domain receptors that couple to G-proteins. |
2(0,0,0,2) | Details |
| 11564657 | Berg KA, Cropper JD, Niswender CM, Sanders-Bush E, Emeson RB, Clarke WP: RNA-editing of the 5-HT (2C) receptor alters agonist-receptor-effector coupling specificity. Br J Pharmacol. 2001 Sep;134(2):386-92. G proteins). |
2(0,0,0,2) | Details |
| 16767512 | Pucadyil TJ, Jafurulla M, Chattopadhyay A: Prolonged treatment with ligands affects ligand binding to the human serotonin (1A) receptor in Chinese hamster ovary cells. Cell Mol Neurobiol. 2006 May;26(3):247-57. Epub 2006 Apr 21. The serotonin (1A) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins, and appear to be involved in several behavioral and cognitive functions. 2. |
2(0,0,0,2) | Details |
| 11426831 | Quirk K, Lawrence A, Jones J, Misra A, Harvey V, Lamb H, Revell D, Porter RH, Knight AR: Characterisation of agonist binding on human 5-HT2C receptor isoforms. Eur J Pharmacol. 2001 May 11;419(2-3):107-12. The VSV isoform lacks the high affinity recognition site for which may be caused by low efficiency coupling to G-proteins. In these studies the affinity of agonists Ro600175 ((S)-2-(6-Chloro-5-fluoroindol-1-yl)-1-methylethylamine), MK212 (6-Chloro-2-(piperazinyl) pyrazine), mCPP (1-(m-chlorophenyl)-piperazine), TfMPP (N-(m-trifluoromethylphenyl) piperazine), DOI (1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane), DOB (1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane) and 8OH-DPAT (8-hydroxy-2-(di-N-propylamino) tetralin) was higher at the INI isoform, whilst antagonist affinity (ketanserin and mesulergine) did not change between the two receptor isoforms. |
2(0,0,0,2) | Details |
| 12769714 | Boyle CD, Palani A: Structure-activity relationship studies: M2 and CCR5 receptor antagonists. . Curr Top Med Chem. 2003;3(10):1155-69. A wide range of neurotransmitters, polypeptides and inflammatory mediators transduce their signals into the interior of cell by specific interactions with cell-surface receptors that are coupled to G-protein. |
2(0,0,0,2) | Details |
| 14556235 | Oz M, Zhang L, Rotondo A, Sun H, Morales M: Direct activation by of recombinant human 5-HT1A receptors: comparison with human 5-HT2C and 5-HT3 receptors. Synapse. 2003 Dec 15;50(4):303-13. Application of or DA in oocytes coexpressing 5-HT1A receptors and G-protein-activated inwardly rectifying channels (GIRK1) induced inward currents with respective EC50 values of 4.2 nM and 11.2 microM. Magnitudes of maximal DA induced currents were 42 +/- 3% of maximal responses and blocked by the 5-HT2 antagonist, piperazine (1 microM). |
1(0,0,0,1) | Details |
| 18190908 | Heusler P, Newman-Tancredi A, Loock T, Cussac D: Antipsychotics differ in their ability to internalise human D2S and human 5-HT1A receptors in HEK293 cells. Eur J Pharmacol. 2008 Feb 26;581(1-2):37-46. Epub 2007 Nov 28. Interestingly, the internalisation induced by clozapine was only minimal, whereas aripirazole and bifeprunox were more potent for internalisation than for G-protein activation. Among antipsychotics with combined D (2)/5-HT (1A) properties, bifeprunox and (3-exo)-8-benzoyl-N-[[(2S) 7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl] methyl ]-8-azabicyclo-[3.2.1] -3- (SSR181507) partially internalised HA-hD (2S) receptors, piperazine, 1-(2,3-dihydro-1,4-benzodioxin-5-yl)-4-[[5-(4-fluorophenyl)-3-pyridinyl] me thyl (SLV313) and N-[(2,2-dimethyl-2,3-dihydro-benzofuran-7-yloxy) ethyl]-3-(cyclopent-1-enyl )-benzylamine (F15063) were inactive. |
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. The maximum response for S 14506 in these assays was equivalent to indicating it to be a full agonist.In molecular modelling studies, using a three-site model of the 5-HT (1A) receptor, S 14506 spanned between the recognition site and the switch" (DRY microdomain) postulated to activate the interaction of the receptor with the G protein. |
1(0,0,0,1) | 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. 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. Furthermore, LY228,729, S14506, and (+)-8-OH-DPAT induce a potent and efficacious coupling of the 5-HT (1A)-D116A receptor to G protein activation as measured by Ca (2+) mobilization and 5'-O-(3-[(35) S] thio) binding in Chinese hamster ovary cells as well as by G protein-coupled inwardly rectifying potassium channel current activation in Xenopus laevis oocytes. |
1(0,0,0,1) | Details |
| 11159702 | Newman-Tancredi A, Verriele L, Millan MJ: Differential modulation by GTPgammaS of agonist and inverse agonist binding to h5-HT (1A) receptors revealed by [3H]-WAY100,635. Br J Pharmacol. 2001 Jan;132(2):518-24. GTPgammaS-induced affinity changes of agonist and inverse agonist competition isotherms generally correlate well with ligand efficacy, with the notable exception of two chemically-similar agents, S14506 and S14671, which are efficacious agonists, yet relatively insensitive to h5-HT (1A) receptor/G-protein coupling changes. |
1(0,0,0,1) | Details |
| 15254141 | Chiou LC, Chuang KC, Wichmann J, Adam G: Ro 64-6198 [(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaz a-spiro [4.5] decan-4-one] acts differently from nociceptin/orphanin FQ in rat periaqueductal gray slices. J Pharmacol Exp Ther. 2004 Nov;311(2):645-51. Epub 2004 Jul 13. Ro 64-6198, like N/OFQ, activated G protein-coupled inwardly rectifying K (+) channels (GIRK) in ventrolateral PAG neurons but displayed only 60% efficacy and 22% potency of N/OFQ. The effect of Ro 64-6198 was not affected by naloxone (1 microM), sulpiride (10 microM), and [1-(2-methoxyphenyl)-4-[4-2-phthalimido) butyl] piperazine (NAN-190) (1 microM), respectively, the antagonist of opioid, D (2), and 5-HT (1A) receptors. |
1(0,0,0,1) | Details |
| 11728188 | Perrone R, Berardi F, Colabufo NA, Leopoldo M, Lacivita E, Tortorella V, Leonardi A, Poggesi E, Testa R: trans-4-[4-(Methoxyphenyl) cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT (1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl) propyl]-1-arylpiperazine s. J Med Chem. 2001 Dec 6;44(25):4431-42. Among the new derivatives emerged trans-4-[4-(3-methoxyphenyl) cyclohexyl]-1-(2-pyridinyl) piperazine (trans-8a) and trans-N-[4-(3-methoxyphenyl) cyclohexyl]-2-(2-pyridyloxy) ethylamine (trans-8b). They were also submitted to the [35S] GTPgammaS binding assay stimulating the 5-HT1A receptor-mediated G-protein activation, therefore behaving as full or as partial agonists. |
1(0,0,0,1) | Details |
| 11747364 | Rieck PW, Cholidis S, Hartmann C: Intracellular signaling pathway of FGF-2-modulated corneal endothelial cell migration during wound healing in vitro. Exp Eye Res. 2001 Nov;73(5):639-50. In different experiments, cells were incubated with either FGF-2 (10 ng ml (-1)), pertussis toxin (PTX; 1-50 ng ml (-1)), phorbol 12- 13- (PMA; 50 ng ml (-1)), 2,4'-di-bromoacetophenone (DAP; 5 microM), 1-(5-iosquinolinesulphonyl)-2-methyl-piperazine dihydrochloride (H7; 10 microM), indomethacin (5 ng ml (-1)), nordihydroguaiaretic acid (NDGA; 10 ng ml (-1)), 2-(4-morpholinyl)-8-pheny-4H-1-benzopyran-4-one (LY294002; 10 microM) or different combinations of these agents. |
0(0,0,0,0) | Details |