| Name | yl 1 |
|---|---|
| Synonyms | Protein YL 1; Swc2; TCFL 1; TCFL1; Transcription factor like 1; Transformation suppressor gene YL 1; VPS72; Vacuolar protein sorting associated protein 72 homolog… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 12734389 | Hajos M, Hoffmann WE, Weaver RJ: Regulation of septo-hippocampal activity by 5-hydroxytryptamine (2C) receptors. J Pharmacol Exp Ther. 2003 Aug;306(2):605-15. Epub 2003 May 6. Intravenous administration of 5-HT2C receptor agonists 1-(3-chlorophenyl) piperazine dihydrochloride (m-CPP) and [S]-2-(chloro-5--indol-1-yl)-1-methyl-ethylamine (Ro 60-0175) dose dependently inhibited firing activity most of the recorded MS/DBv neurons and abolished theta oscillation in all tested MS/DBv and hippocampal neurons. |
31(0,1,1,1) | Details |
| 16161996 | Rudolf K, Eberlein W, Engel W, Pieper H, Entzeroth M, Hallermayer G, Doods H: Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. J Med Chem. 2005 Sep 22;48(19):5921-31. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2 (1H)-oxoquinazolin-3-yl)-1-piperidi nyl] carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl) piperazine: the first CGRP antagonist for clinical trials in acute migraine.. |
31(0,1,1,1) | Details |
| 19193935 | Guard DB, Swartz TD, Ritter RC, Burns GA, Covasa M: Blockade of hindbrain NMDA receptors containing NR2 subunits increases intake. Am J Physiol Regul Integr Comp Physiol. 2009 Apr;296(4):R921-8. Epub 2009 Feb 4. To test this, we measured deprivation-induced intake of 15% solution following fourth ventricle and intra-nucleus of the solitary tract (intra-NTS) injections of Conantokin G (Con G; NR2B blocker), d-3-(2-carboxypiperazin-4-yl)-1-propenyl-1- (d-CPPene; NR2B/2A blocker), and (+/-)-cis-1-(phenanthren-2yl-carbonyl) piperazine-2,3-dicarboxylic acid (PPDA; NR2D/C blocker). |
6(0,0,1,1) | 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. 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. |
2(0,0,0,2) | Details |
| 15080922 | Upadhayaya RS, Sinha N, Jain S, Kishore N, Chandra R, Arora SK: Optically active antifungal azoles: synthesis and antifungal activity of (2R,3S)-2-(2,4-difluorophenyl)-3-(5-[2-[4-aryl-piperazin-1-yl]-ethyl]-tetr azol-2-yl/1-yl)-1-[1,2,4]-triazol-1-yl-butan-2-ol. Bioorg Med Chem. 2004 May 1;12(9):2225-38. Compounds 11d and its positional isomer 12d having 3-trifluoromethyl substitution on the phenyl ring of piperazine demonstrated significant antifungal activity against variety of fungal cultures (Candida spp. |
2(0,0,0,2) | Details |
| 17649988 | Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R: Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21. Epub 2007 Jul 25. Here we report the synthesis of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides 16-29 that were designed to elucidate both structure-affinity and -activity relationships for the 5-HT7 receptor, by targeting the substituent in 2-position of the aryl linked to the piperazine ring. Certain lipophilic substituents (SCH3, CH (CH3) 2, N (CH3) 2, CH3, Ph) led to high-affinity agonists, whereas OH and NHCH3 substituents switched intrinsic activity toward antagonism. 4-[2-(1-Methylethyl) phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-pipera zinehexanamide (19), 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexanamid e (21), and 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazi nehexanamide (22) were identified as potent 5-HT7 receptor agonists (Ki = 0.13-1.1 nM, EC50 = 0.90-1.77 microM), showing selectivity over 5-HT1A, 5-HT2A, and D2 receptors. |
1(0,0,0,1) | Details |
| 15336263 | Heinrich T, Bottcher H, Schiemann K, Holzemann G, Schwarz M, Bartoszyk GD, van Amsterdam C, Greiner HE, Seyfried CA: Dual 5-HT1A agonists and re-uptake inhibitors by combination of -butyl-amine and chromenonyl-piperazine structural elements in a single molecular entity. Bioorg Med Chem. 2004 Sep 15;12(18):4843-52. In the course of structural modifications of vilazodone 3-[4-[4--6-yl)-1-piperazinyl]-butyl]-1H-indole-5-car 8i and its analogue 6-[4-[4-(5-fluor-3-indolyl)-butyl]-1-piperazinyl]- have been identified. |
1(0,0,0,1) | Details |
| 18582863 | Kimura Y, Naitou Y, Wanibuchi F, Yamaguchi T: 5-HT (2C) receptor activation is a common mechanism on proerectile effects of apomorphine, and melanotan-II in rats. Eur J Pharmacol. 2008 Jul 28;589(1-3):157-62. Epub 2008 May 24. SB200646 at 10 mg/kg and SB242084 at 3 mg/kg, these doses which completely antagonize penile erections induced by 5-HT (2C) receptor agonists, m-chlorophenylpiperazine (mCPP) and (S)-2-(7-ethyl-1H-furo [2,3-g] indazol-1-yl)-1-methylethylamine (YM348), significantly inhibited penile erections elicited by apomorphine, or MT-II. |
1(0,0,0,1) | Details |
| 15588097 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Niso M, Perrone R, Tortorella V: Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. J Med Chem. 2004 Dec 16;47(26):6616-24. In relation to 5-HT7 receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role. Among them, 4-(2-methoxyphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexa namide (28), 4-(2-acetylphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexan amide (34), 4-(2-methylthiophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazineh exanamide (44), 4-(2-hydroxyphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexa namide (46), and 4-(2-methylphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazinehexan amide (49) were assayed for the 5-HT7 receptor-mediated relaxation of substance P-induced guinea pig ileum contraction. |
1(0,0,0,1) | Details |
| 11509227 | Vickers SP, Easton N, Malcolm CS, Allen NH, Porter RH, Bickerdike MJ, Kennett GA: Modulation of 5-HT (2A) receptor-mediated head-twitch behaviour in the rat by 5-HT (2C) receptor agonists. Pharmacol Biochem Behav. 2001 Jul-Aug;69(3-4):643-52. The preferential 5-HT (2C) receptor agonists Ro 60-0175, 6-chloro-2-[1-piperazinyl]-pyrazine HCl (MK-212), 1-(3-chlorophenyl) piperazine hydrochloride (mCPP), 1-(3-trifluoromethylphenyl) piperazine hydrochloride (TFMPP), and (S)-3-[(2,3-dihydro-5-methoxy-1H-inden-4-yl) oxy]-pyrollidine HCl (ORG-37684), the 5-HT (2A/2C) receptor agonist 2,5-dimethoxy-4-iodoamphetamine (DOI), the 5-HT (2B) receptor agonist 1-[5-thienylmethoxy-1-1H-3-indoyl] propan-2-amine hydrochloride (BW-723C86), and nor-D-fenfluramine were administered to rats subsequent to an acute challenge of SB-242084. |
0(0,0,0,0) | Details |
| 15719229 | Hayashi A, Suzuki M, Sasamata M, Miyata K: Agonist diversity in 5-HT (2C) receptor-mediated weight control in rats. Psychopharmacology. 2005 Mar;178(2-3):241-9. Epub 2004 Oct 21. OBJECTIVES: The purpose of the present study was to investigate the effect of repeated oral administration of three 5-HT (2C) receptor agonists, m-chlorophenylpiperazine (mCPP), d (S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine (RO60-0175) and (S)-2-(7-ethyl-1H-furo [2,3-g] indazol-1-yl)-1-methylethylamine (YM348), on food intake and energy expenditure in rats. |
1(0,0,0,1) | Details |
| 12723957 | Osa Y, Kobayashi S, Sato Y, Suzuki Y, Takino K, Takeuchi T, Miyata Y, Sakaguchi M, Takayanagi H: Structural properties of dibenzosuberanylpiperazine derivatives for efficient reversal of chloroquine resistance in Plasmodium chabaudi. J Med Chem. 2003 May 8;46(10):1948-56. For the purpose of developing chemosensitizers to reverse chloroquine (CQ) resistance in Plasmodium chabaudi in vivo, dibenzosuberanylpiperazine (1-(10,11-dihydro-5H-dibenzo [a,d] cyclohepten-5-yl) piperazine) (DSP) and its piperazin-1-yl derivatives were synthesized systematically. |
0(0,0,0,0) | 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. 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. |
0(0,0,0,0) | Details |
| 15146031 | Millan MJ, Gobert A, Roux S, Porsolt R, Meneses A, Carli M, Di Cara B, Jaffard R, Rivet JM, Lestage P, Mocaer E, Peglion JL, Dekeyne A: The serotonin1A receptor partial agonist S15535 [4-(benzodioxan-5-yl) 1-(indan-2-yl) piperazine] enhances cholinergic transmission and cognitive function in rodents: a combined neurochemical and behavioral analysis. J Pharmacol Exp Ther. 2004 Oct;311(1):190-203. Epub 2004 May 14. |
62(0,2,2,2) | Details |
| 18404460 | Gessi S, Varani K, Merighi S, Leung E, Mac Lennan S, Baraldi PG, Borea PA: Novel selective antagonist radioligands for the pharmacological study of A (2B) receptors. Purinergic Signal. 2006 Nov;2(4):583-8. Epub 2006 Jul 8. Recently, high-affinity radioligands for A (2B) receptors, [N-(4-cyanophenyl)-2-[4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-puri n-8-yl)-phenoxy] acetamide ([(3) H] MRS 1754), N-(2-(2-Phenyl-6-[4-(2,2,3,3-tetratritrio-3-phenylpropyl)-piperazine-1-car bonyl]-7H-pyrrolo [2,3-d] pyrimidin-4-ylamino)-ethyl)-acetamide ([(3) H] OSIP339391) and N-benzo [1,3] dioxol-5-yl-2-[5-(1,3-dipropyl-2,6-dioxo-2,3,6,7-tetrahydro-1H -purin-8-yl)-1-methyl-1H-pyrazol-3-yloxy]-acetamide] ([(3) H] MRE 2029F20), have been introduced. |
31(0,1,1,1) | Details |
| 18271296 | Bharathi Ch, Prabahar KJ, Prasad ChS, Srinivasa Rao M, Trinadhachary GN, Handa VK, Dandala R, Naidu A: Identification, isolation, synthesis and characterization of impurities of Pharmazie. 2008 Jan;63(1):14-9. Based on the spectral data, the impurities were characterized as 2-[4-dibenzo [b,f][1,4] thiazepine-11-yl-1 -piperazinyl] 1 -2- (impurity I, desethanol 11-[(N-formyl)-1-piperazinyl]-dibenzo [b,f][1,4] thiazepine (impurity II, N-formyl piperazinyl thiazepine), 2-(2- ethoxy) ethyl-2-[2-[4-dibenzo [b,f][1,4] thiazepine-11- piperazinyl-1-carboxylate (impurity III, carboxylate), 11-[4-ethyl-1-piperazinyl] dibenzo [b,f][1,4] thiazepine (impurity IV, ethylpiperazinyl thiazepine), 2-[2-(4-dibenzo [b,f][1,4] thiazepin-11-yl-1-piperazinyl) ethoxy] 1-ethyl [impurity V, ethyl 1,4-bis [dibenzo [b,f][1,4] thiazepine-11-yl] piperazine [impurity VI, bis (dibenzo) piperazine]. |
31(0,1,1,1) | 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. 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. |
31(0,1,1,1) | 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. 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. |
31(0,1,1,1) | Details |
| 16289351 | Gannon RL, Millan MJ: Serotonin1A autoreceptor activation by S 15535 enhances circadian activity rhythms in hamsters: evaluation of potential interactions with serotonin2A and serotonin2C receptors. Neuroscience. 2006;137(1):287-99. Epub 2005 Nov 10. In contrast, the (5HT) 1A partial agonist, 4-(benzodioxan-5-yl) 1-(indan2-yl) piperazine (S 15535), was found to enhance the phase-shifting influence of light on hamster circadian rhythms [Gannon, Neuroscience 119 (2003) 567]. |
31(0,1,1,1) | Details |