PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 27358233-1 2017 N-Benzylpiperazine (BZP) and 1-(3-trifluoromethylphenyl)piperazine (TFMPP) are two synthetic phenylpiperazine analogues that have been frequently commercialized in combination as an alternative to ecstasy ("Legal X"). phenylpiperazine 93-109 zinc finger E-box binding homeobox 1 Homo sapiens 20-23 27658794-0 2016 Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents. phenylpiperazine 13-29 prostaglandin-endoperoxide synthase 2 Homo sapiens 74-79 25648298-0 2015 Discovery of phenylpiperazine derivatives as IGF-1R inhibitor with potent antiproliferative properties in vitro. phenylpiperazine 13-29 insulin like growth factor 1 receptor Homo sapiens 45-51 26349898-0 2015 Discovery of a series of novel phenylpiperazine derivatives as EGFR TK inhibitors. phenylpiperazine 31-47 epidermal growth factor receptor Homo sapiens 63-67 26349898-2 2015 We report herein the discovery of a novel class of phenylpiperazine derivatives with improved potency toward EGFR. phenylpiperazine 51-67 epidermal growth factor receptor Homo sapiens 109-113 25648298-5 2015 These studies confirmed that these new phenylpiperazine derivatives maintain their mechanisms of action by disrupting IGF-1R kinase. phenylpiperazine 39-55 insulin like growth factor 1 receptor Homo sapiens 118-124 24211020-2 2013 In the course of our studies to determine the optimal substituents in the sigma2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand. phenylpiperazine 91-109 solute carrier family 6 member 3 Homo sapiens 288-309 24211020-2 2013 In the course of our studies to determine the optimal substituents in the sigma2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand. phenylpiperazine 91-109 solute carrier family 6 member 3 Homo sapiens 311-314 24211020-2 2013 In the course of our studies to determine the optimal substituents in the sigma2-selective phenyl piperazines analogues with reduced activity at other neurotransmitter systems, we discovered that 1-(3-chlorophenyl)-4-phenethylpiperazine actually had preferentially increased affinity for dopamine transporters (DAT), yielding a highly selective DAT ligand. phenylpiperazine 91-109 solute carrier family 6 member 3 Homo sapiens 345-348 23019496-2 2012 Drugs of abuse such as MDMA (streetname "ecstasy") and certain 1-phenyl-piperazine (PP) analogs such as 1-(3-chlorophenyl)-piperazine (mCPP) elicit their stimulatory effect by elevating the synaptic concentration of serotonin by blocking or reversing the normal transport activity of hSERT. phenylpiperazine 63-82 solute carrier family 6 member 4 Homo sapiens 284-289 23766142-0 2013 Fos expression in response to dopamine D3-preferring phenylpiperazine drugs given with and without cocaine. phenylpiperazine 53-69 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 0-3 21602603-5 2011 The pharmacologically active compounds 9-11 with the phenylpiperazine moiety showed affinity for alpha(1)-receptors (K(i) = 0.143-0.383 muM), but the other compounds were almost (12-15) or completely (8) inactive at this site. phenylpiperazine 53-69 latexin Homo sapiens 136-139 21721047-4 2011 However, the phenylpiperazine linker group was dramatically more mobile in Mcl-1 compared to either Bcl-x(L) or Bcl-2. phenylpiperazine 13-29 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 75-80 21721047-4 2011 However, the phenylpiperazine linker group was dramatically more mobile in Mcl-1 compared to either Bcl-x(L) or Bcl-2. phenylpiperazine 13-29 BCL2 apoptosis regulator Homo sapiens 112-117 21163968-7 2011 Targeted chemical modification of the phenylpiperazine moiety at the site of its interaction with the residue His393(6.55) led to the functionally selective ligand {3-[4-(2,3-dihydro-benzofuran-7-yl)-piperazin-1-yl]-propyl}-pyrazol[1,5-a]pyridine-3-carboxamide (FAUC350) that has distinct signaling profiles toward adenylyl cyclase and ERK1/2. phenylpiperazine 38-54 mitogen-activated protein kinase 3 Homo sapiens 336-342 19388677-1 2009 In an effort to discover novel druglike NK(1) receptor antagonists a new series of suitably substituted C-phenylpiperazine derivatives was identified by an appropriate chemical exploration of related N-phenylpiperazine analogues, with the specific aim to maximize their in vitro affinity and optimize in parallel their pharmacokinetic profile. phenylpiperazine 200-218 tachykinin receptor 1 Homo sapiens 40-54 16412632-0 2006 BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline. phenylpiperazine 48-65 beta-secretase 1 Homo sapiens 0-6 18220971-0 2008 Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists. phenylpiperazine 69-86 melanocortin 4 receptor Homo sapiens 90-113 17994683-0 2007 Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor. phenylpiperazine 61-78 melanocortin 4 receptor Mus musculus 147-170 18082872-1 2008 Previous studies have demonstrated that LASSBio-579 and LASSBio-581, two N-phenylpiperazine derivatives designed for the treatment of schizophrenia, are presynaptic dopamine D(2) receptor agonists that induce a hypothermic effect in mice that is not mediated by dopamine receptor activation. phenylpiperazine 73-91 dopamine receptor D2 Mus musculus 165-187 18037910-8 2008 The guinea pig P2X(7) receptor possessed higher affinity for 1-[N,O-bis(5-isoquinoline sulphonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine (KN62), suramin and Coomassie Brilliant Blue than human or rat P2X(7) receptors suggesting that it is pharmacologically different to other rodent or human P2X(7) receptors. phenylpiperazine 119-136 purinergic receptor P2X, ligand-gated ion channel, 7 Mus musculus 15-30 17585854-5 2007 The most potent P2X7 receptor antagonist identified in this study (compound 4g) contains an o-fluorine substituent on the phenylpiperazine moiety and had an IC50 of 12.1 nM. phenylpiperazine 122-138 purinergic receptor P2X 7 Homo sapiens 16-29 16919461-0 2006 Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives. phenylpiperazine 103-119 neuropeptide Y receptor Y5 Homo sapiens 28-39 16919461-1 2006 A series of phenylpiperazine derivatives were synthesized and evaluated for their neuropeptide Y (NPY) Y5 receptor antagonistic activities. phenylpiperazine 12-28 neuropeptide Y receptor Y5 Homo sapiens 82-114 16919461-3 2006 Subsequent optimization of the phenylpiperazine template by substitution of the phenyl moiety resulted in a series of (2-methanesulfonamidephenyl)piperazine derivatives that showed potent binding affinity and antagonistic activity for the Y5 receptor. phenylpiperazine 31-47 neuropeptide Y receptor Y5 Homo sapiens 239-250 16412632-2 2006 Here, we report a new series of analogues based on the phenyl-piperazine scaffold coupled to various heterocyclic moieties, which demonstrate improved inhibitory activities on BACE-1 (FRET assay) compared to already known naphthyl counterparts. phenylpiperazine 55-72 beta-secretase 1 Homo sapiens 176-182 11670871-11 1999 Complex 8, (CuCN)(phpip), crystallizes in the monoclinic space group P2(1)/cwith unit cell dimensions a = 17.8819(3) A, b = 6.9190(1) A, c = 8.6972(1) A, beta = 96.720(1) degrees, and Z = 4. phenylpiperazine 18-23 cyclin-dependent kinase inhibitor 1A (P21) Mus musculus 69-74 14552781-1 2003 Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC(50)=24 nM) and selective MC4-R agonists. phenylpiperazine 29-46 melanocortin 4 receptor Homo sapiens 184-189 15107597-1 2003 Our aim was to specify the 5-HT(2) subtype selectivity of EGIS-7625 (1-benzyl-4-[(2-nitro-4-methyl-5-amino)-phenyl]-piperazine), a new 5-HT(2B) ligand, in receptor binding studies and characterize its pharmacology at 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors in in vivo experiments and in isolated organs, in vitro. phenylpiperazine 106-126 5-hydroxytryptamine receptor 2B Homo sapiens 135-142 12204476-1 2002 Compounds in which N-phenylpiperazines were linked by a propyloxy chain to position 6 or 7 of a coumarin ring were designed and synthesised, and their affinities for 5-HT(1A) and D(2A) receptors were determined by radioligand binding assays. phenylpiperazine 19-38 5-hydroxytryptamine receptor 1A Homo sapiens 166-173 10853650-0 2000 Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. phenylpiperazine 6-22 tumor necrosis factor Mus musculus 68-77 10853650-0 2000 Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. phenylpiperazine 6-22 interleukin 10 Mus musculus 94-99 10853650-1 2000 Phenylpiperazine derivatives were synthesized as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. phenylpiperazine 0-16 tumor necrosis factor Mus musculus 79-88 10853650-1 2000 Phenylpiperazine derivatives were synthesized as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. phenylpiperazine 0-16 interleukin 10 Mus musculus 105-110 10397500-2 1999 A test series of 32 phenylpiperazines III with affinity for 5-HT1A and alpha1 receptors was subjected to QSAR analysis using artificial neural networks (ANNs), in order to get insight into the structural requirements that are responsible for 5-HT1A/alpha1 selectivity. phenylpiperazine 20-37 5-hydroxytryptamine receptor 1A Homo sapiens 60-66 10397500-2 1999 A test series of 32 phenylpiperazines III with affinity for 5-HT1A and alpha1 receptors was subjected to QSAR analysis using artificial neural networks (ANNs), in order to get insight into the structural requirements that are responsible for 5-HT1A/alpha1 selectivity. phenylpiperazine 20-37 5-hydroxytryptamine receptor 1A Homo sapiens 242-248 11888550-0 2002 Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. phenylpiperazine 89-105 5-hydroxytryptamine receptor 1B Rattus norvegicus 32-39 11170629-2 2001 A classical quantitative structure-activity relationship (Hansch) study and artificial neural networks (ANNs) have been applied to a training set of 32 substituted phenylpiperazines with affinity for 5-HT(1A) and alpha(1)-adrenergic receptors, to evaluate the structural requirements that are responsible for 5-HT(1A)/alpha(1) selectivity. phenylpiperazine 164-181 5-hydroxytryptamine receptor 1A Homo sapiens 200-207 9513604-2 1998 The structural contributions to D2/D3 and 5-HT1A receptor binding of the aminopyrimidine, cycloalkyl, and phenylpiperazine portions of the molecule were examined. phenylpiperazine 106-122 immunoglobulin heavy diversity 2-15 Homo sapiens 32-48 34536431-10 2022 In conclusion, oral administration of the newly synthesized phenylpiperazines produced anxiolytic- and antidepressant-like effects in behavioral tests, putatively in part through the activation of 5-HT1A receptors. phenylpiperazine 60-77 5-hydroxytryptamine (serotonin) receptor 1A Mus musculus 197-203 9364416-0 1997 Synthesis of several substituted phenylpiperazines behaving as mixed D2/5HT1A ligands. phenylpiperazine 33-50 5-hydroxytryptamine receptor 1A Bos taurus 72-77 8960552-2 1996 The synthesis of 1-phenylpiperazines, linked in the alpha or beta position of the tetralin moiety on the terminal part of the N-4 alkyl chain, and their radioligand binding affinities for 5-HT(1A), 5-HT(2A), D-1, D-2, alpha1, and alpha2 receptors along with SAR studies on the 5-HT(1A) receptor are reported. phenylpiperazine 17-36 5-hydroxytryptamine receptor 1A Homo sapiens 188-195 8960552-2 1996 The synthesis of 1-phenylpiperazines, linked in the alpha or beta position of the tetralin moiety on the terminal part of the N-4 alkyl chain, and their radioligand binding affinities for 5-HT(1A), 5-HT(2A), D-1, D-2, alpha1, and alpha2 receptors along with SAR studies on the 5-HT(1A) receptor are reported. phenylpiperazine 17-36 5-hydroxytryptamine receptor 2A Homo sapiens 200-205 8960552-2 1996 The synthesis of 1-phenylpiperazines, linked in the alpha or beta position of the tetralin moiety on the terminal part of the N-4 alkyl chain, and their radioligand binding affinities for 5-HT(1A), 5-HT(2A), D-1, D-2, alpha1, and alpha2 receptors along with SAR studies on the 5-HT(1A) receptor are reported. phenylpiperazine 17-36 5-hydroxytryptamine receptor 1A Homo sapiens 277-294 8960552-4 1996 The highest affinity (IC50 = 0.50 nM) and selectivity for the 5-HT(1A) receptor were showed by 1-phenylpiperazine 2a with a three-membered alkyl chain bearing a 5-methoxytetralin-1-yl ring in the omega position. phenylpiperazine 95-113 5-hydroxytryptamine receptor 1A Homo sapiens 62-79 8923668-1 1996 The in vivo imaging of a novel iodinated phenylpiperazine derivative for 5-HT1A receptors, [123I]p-MPPI (4-(2"-methoxy-)phenyl-1-[2"-(n-2"-pyridinyl)-p-iodobenzamido-] ethyl-piperazine), using single photon emission computed tomography (SPECT), was evaluated in nonhuman primates. phenylpiperazine 41-57 5-hydroxytryptamine receptor 1A Homo sapiens 73-79 8767112-3 1996 It has also been found that the two 1-phenylpiperazine derivatives 32 and 36 are new selective 5-HT2A receptor ligands (Ki = 34 and 37 nM, respectively), whereas the derivative of 1-(o-methoxyphenyl)piperazine (38) is a new, highly potent 5-HT1A receptor ligand (Ki = 0.51 nM) with a moderate affinity for 5-HT2A receptors (Ki = 213 nM). phenylpiperazine 36-54 5-hydroxytryptamine receptor 2A Homo sapiens 95-110 8767112-3 1996 It has also been found that the two 1-phenylpiperazine derivatives 32 and 36 are new selective 5-HT2A receptor ligands (Ki = 34 and 37 nM, respectively), whereas the derivative of 1-(o-methoxyphenyl)piperazine (38) is a new, highly potent 5-HT1A receptor ligand (Ki = 0.51 nM) with a moderate affinity for 5-HT2A receptors (Ki = 213 nM). phenylpiperazine 36-54 5-hydroxytryptamine receptor 2A Homo sapiens 97-101 9436302-0 1997 Structure and serotonin 5-HT2C receptor activity of ortho- and meta-substituted phenylpiperazines. phenylpiperazine 80-97 5-hydroxytryptamine receptor 2C Homo sapiens 14-39 9436302-1 1997 The structural characteristics of ortho- and meta-substituted phenylpiperazines have been investigated in order to understand their actions at the serotonin 5-HT2C receptor. phenylpiperazine 62-79 5-hydroxytryptamine receptor 2C Homo sapiens 147-172 9436302-4 1997 The activities of several phenylpiperazines, in combination with their crystal structures and conformational characteristics, lead to the hypothesis that the conformation for which the piperazine ring and the phenyl ring are approximately co-planar should be the 5-HT2C receptor "activating" conformation. phenylpiperazine 26-43 5-hydroxytryptamine receptor 2C Homo sapiens 263-269 9105540-7 1997 Derivatives of 1-(2-pyridyl)piperazine 1b and 2a and of 1-phenylpiperazine 1a expressed moderate to low affinity for both D-2 and 5-HT1A receptors, while 1-(2-pyridyl)-piperazines 3b and 4b and 4-(1-phenylethyl)-1-(1-naphthyl)-piperazine 10 were moderate [3H]spiperone, but potent 8-OH-[3H]DPAT competitors. phenylpiperazine 56-74 5-hydroxytryptamine receptor 1A Bos taurus 130-136 8951963-4 1996 On the other hand, long-term treatment with the monoamine oxidase type-A inhibiting antidepressant, clorgyline (1 mg/kg/day) and the alpha 2-noradrenergic antagonists, yohimbine and 1-phenylpiperazine (1 mg/kg/day, each) did not modify clonidine"s effect. phenylpiperazine 182-200 monoamine oxidase A Rattus norvegicus 48-72 8748393-2 1995 Three structural classes of compounds have been described to stimulate increases in phosphoinositide (PI) hydrolysis at the 5-HT2C receptor site: phenylpiperazines, phenylalkylamines, and indolamines. phenylpiperazine 146-163 5-hydroxytryptamine receptor 2C Homo sapiens 124-130 8064803-3 1994 Structure-affinity relationship (SAR) studies for the 5-HT1A receptor site are presented for two series of heterobicyclic phenylpiperazines with N4-aralkyl substituents: 4-aralkyl derivatives of 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine (3) and 1-(benzo[b]furan-7-yl)piperazine (4). phenylpiperazine 122-139 5-hydroxytryptamine receptor 1A Homo sapiens 54-69 8365456-1 1993 The novel phenylpiperazine derivative, (+/-)-WAY100135 (N-tert-butyl-3-(4-(2-methoxyphenyl)piperazin-1-yl)-2-phenylpro pionamide dihydrochloride), is a selective antagonist at both somatodendritic and postsynaptic 5-HT1A receptors. phenylpiperazine 10-26 5-hydroxytryptamine receptor 1A Rattus norvegicus 214-220 3982214-0 1985 5-HT-1a and 5-HT-1b selectivity of two phenylpiperazine derivatives: evidence for 5-HT-1b heterogeneity. phenylpiperazine 39-55 5-hydroxytryptamine receptor 1A Rattus norvegicus 0-7 34604625-0 2021 Molecular Dynamics Simulations Identify Tractable Lead-like Phenyl-Piperazine Scaffolds as eIF4A1 ATP-competitive Inhibitors. phenylpiperazine 60-77 eukaryotic translation initiation factor 4A1 Homo sapiens 91-97 34073405-0 2021 Evaluation of Substituted N-Phenylpiperazine Analogs as D3 vs. D2 Dopamine Receptor Subtype Selective Ligands. phenylpiperazine 26-44 dopamine receptor D2 Homo sapiens 63-83 34073405-1 2021 N-phenylpiperazine analogs can bind selectively to the D3 versus the D2 dopamine receptor subtype despite the fact that these two D2-like dopamine receptor subtypes exhibit substantial amino acid sequence homology. phenylpiperazine 0-18 dopamine receptor D2 Homo sapiens 69-89 22156500-1 1989 The new phenylpiperazine derivative flesinoxan, a potent and selective serotonin(1A) (5-HT(1A)) agonist, was examined under a procedure that has proved to be a reliable and sensitive method for detecting novel anxiolytic drugs believed to produce their effects at the 5-HT( 1A) receptor subtype. phenylpiperazine 8-24 5-hydroxytryptamine receptor 1A Homo sapiens 86-93 22156500-1 1989 The new phenylpiperazine derivative flesinoxan, a potent and selective serotonin(1A) (5-HT(1A)) agonist, was examined under a procedure that has proved to be a reliable and sensitive method for detecting novel anxiolytic drugs believed to produce their effects at the 5-HT( 1A) receptor subtype. phenylpiperazine 8-24 5-hydroxytryptamine receptor 1A Homo sapiens 268-286 2879202-0 1986 In vitro receptor specificity of the 5HT1A selective phenylpiperazine, LY165163. phenylpiperazine 53-69 5-hydroxytryptamine receptor 1A Rattus norvegicus 37-42 3982214-0 1985 5-HT-1a and 5-HT-1b selectivity of two phenylpiperazine derivatives: evidence for 5-HT-1b heterogeneity. phenylpiperazine 39-55 5-hydroxytryptamine receptor 1B Rattus norvegicus 12-19 3982214-0 1985 5-HT-1a and 5-HT-1b selectivity of two phenylpiperazine derivatives: evidence for 5-HT-1b heterogeneity. phenylpiperazine 39-55 5-hydroxytryptamine receptor 1B Rattus norvegicus 82-89 32086055-2 2020 The compounds exhibited high affinity for the 5-HT1A receptor, (especially 4dKi = 0.4 nM) which depended on the substitution pattern at the phenylpiperazine moiety. phenylpiperazine 140-156 5-hydroxytryptamine receptor 1A Homo sapiens 46-61 32631504-2 2020 Herein we report the discovery of a series of new SIRT6 inhibitors containing the skeleton 1-phenylpiperazine. phenylpiperazine 91-109 sirtuin 6 Mus musculus 50-55 33988991-3 2021 Here, we examine the molecular basis for the high affinity D3R binding and D3R vs D2R binding selectivity of substituted phenylpiperazine thiopheneamides. phenylpiperazine 121-137 dopamine receptor D3 Homo sapiens 75-78 33988991-3 2021 Here, we examine the molecular basis for the high affinity D3R binding and D3R vs D2R binding selectivity of substituted phenylpiperazine thiopheneamides. phenylpiperazine 121-137 dopamine receptor D2 Homo sapiens 82-85 30010318-3 2018 Our goal was to investigate how the composition and size of the nonaromatic ring structure at the piperazine position of substituted phenylpiperazine analogues might influence binding affinity at the human D2 and D3 dopamine receptors. phenylpiperazine 133-149 dopamine receptor D2 Homo sapiens 206-234 31989362-10 2020 Pre-incubation of mucosae with two 5-HT4 receptor antagonists, a loop diuretic and a myosin light chain kinase inhibitor, reduced the permeation enhancement capacity of PPZ and 1-4-MPP for [14C]-mannitol. phenylpiperazine 169-172 myosin light chain kinase Rattus norvegicus 85-110 32560608-2 2020 This study was undertaken to identify if indol-2-carboxylic acid esters containing N-phenylpiperazine moiety possess acetylcholinesterase and butyrylcholinesterase inhibitory activity. phenylpiperazine 83-101 butyrylcholinesterase Homo sapiens 142-163 31214037-1 2019 LASSBio-579, an N-phenylpiperazine antipsychotic lead compound, has been previously reported as a D2 receptor (D2R) ligand with antipsychotic-like activities in rodent models of schizophrenia. phenylpiperazine 16-34 dopamine receptor D2 Homo sapiens 98-109 31214037-1 2019 LASSBio-579, an N-phenylpiperazine antipsychotic lead compound, has been previously reported as a D2 receptor (D2R) ligand with antipsychotic-like activities in rodent models of schizophrenia. phenylpiperazine 16-34 dopamine receptor D2 Homo sapiens 111-114