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Piperazines

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  • 5-HT(1A) receptor binding in the dorsal raphe nucleus is implicated in the anxiolytic-like effects of Cinnamomum cassia  Academic Article
  • 5-HT(1A) receptor mutant mice exhibit enhanced tonic, stress-induced and fluoxetine-induced serotonergic neurotransmission  Academic Article
  • 8-OH-DPAT acts on both 5-HT1A and 5-HT7 receptors to induce hypothermia in rodents  Academic Article
  • A brief review of the past and future of platelet P2Y12 antagonist  Academic Article
  • A conserved salt bridge in the G loop of multiple protein kinases is important for catalysis and for in vivo Lyn function  Academic Article
  • A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity  Academic Article
  • A new class of highly cytotoxic diketopiperazines  Academic Article
  • A nucleophile-catalyzed cycloisomerization permits a concise synthesis of (+)-harziphilone  Academic Article
  • A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors  Academic Article
  • Allosteric inhibitors of Bcr-abl-dependent cell proliferation  Academic Article
  • Alpha-2c-adrenergic receptors contribute to basal nasal patency in the anesthetized cat  Academic Article
  • Antagonism of the histamine H-4 receptor reduces LPS-induced TNF production in vivo  Academic Article
  • Antibody conjugation approach enhances breadth and potency of neutralization of anti-HIV-1 antibodies and CD4-IgG  Academic Article
  • Antidepressant-like effects of albizzia julibrissin in mice: Involvement of the 5-ht1a receptor system  Academic Article
  • Antiobesity effect of a small molecule repressor of RORγ  Academic Article
  • Antitumor effects and mechanisms ofAZD4547on FGFR2-deregulated endometrial cancer cells  Academic Article
  • Anxiogenic effects of nicotine in the dorsal hippocampus are mediated by 5-ht1a and not by muscarinic m-1 receptors  Academic Article
  • Anxiogenic-like effect of serotonin(1B) receptor stimulation in the rat elevated plus-maze  Academic Article
  • Anxiolytic-like effects of sinapic acid in mice  Academic Article
  • Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)  Academic Article
  • Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51  Academic Article
  • CD4-induced activation in a soluble HIV-1 Env trimer  Academic Article
  • Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways  Academic Article
  • Characterization of lassa virus cell entry inhibitors: Determination of the active enantiomer by asymmetric synthesis  Academic Article
  • Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases  Academic Article
  • Chemoproteomic evaluation of target engagement by the cyclin-dependent kinase 4 and 6 inhibitor palbociclib correlates with cancer cell response  Academic Article
  • Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors  Academic Article
  • Cytochrome P450-catalyzed L-tryptophan nitration in thaxtomin phytotoxin biosynthesis  Academic Article
  • Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain  Academic Article
  • Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino) cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methano ne, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile  Academic Article
  • Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist  Academic Article
  • Discovery of PF-00217830: aryl piperazine napthyridinones as D-2 partial agonists for schizophrenia and bipolar disorder  Academic Article
  • Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors  Academic Article
  • Distinct effect of pregnenolone sulfate on NMDA receptor subtypes  Academic Article
  • Distinct mechanisms for spiro-carbon formation reveal biosynthetic pathway crosstalk  Academic Article
  • Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo  Academic Article
  • E2f-1 cooperates with topoisomerase ii inhibition and DNA damage to selectively augment p53-independent apoptosis  Academic Article
  • EPPS rescues hippocampus-dependent cognitive deficits in APP/PS1 mice by disaggregation of amyloid-β oligomers and plaques  Academic Article
  • Effect of aripiprazole, a partial dopamine d-2 receptor agonist, on increased rate of methamphetamine self-administration in rats with prolonged session duration  Academic Article
  • Effects of amperozide, 8-OH-DPAT, and FG 5974 on operant responding for ethanol  Academic Article
  • Endocannabinoid regulation of nausea is mediated by 2-arachidonoylglycerol (2-AG) in the rat visceral insular cortex  Academic Article
  • Exploring aromatic chemical space with NEAT: novel and electronically equivalent aromatic template  Academic Article
  • Galanin stimulates the N-methyl-D-aspartate receptor/nitric oxide/cyclic GMP pathway in vivo in the rat ventral hippocampus  Academic Article
  • Growth arrest of BCR-ABL positive cells with a sequence-specific polyamide-chlorambucil conjugate  Academic Article
  • High affinity targets of protein kinase inhibitors have similar residues at the positions energetically important for binding  Academic Article
  • Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker  Academic Article
  • Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist  Academic Article
  • Identification of SR2211: a potent synthetic ROR gamma-selective modulator  Academic Article
  • Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery  Academic Article
  • Imidazolopiperazines: Hit to lead optimization of new antimalarial agents  Academic Article
  • Imidazolopiperazines: Lead optimization of the second-generation antimalarial agents  Academic Article
  • Impact of serotonin 2C receptor null mutation on physiology and behavior associated with nigrostriatal dopamine pathway function  Academic Article
  • Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection  Academic Article
  • Inactivation of the p53 pathway in retinoblastoma  Academic Article
  • Inhibition of adenovirus replication by a trisubstituted piperazin-2-one derivative  Academic Article
  • Investigations on the 1-(2-biphenyl)piperazine motif: Identification of new potent and selective ligands for the serotonin(7) (5-ht7) receptor with agonist or antagonist action in vitro or ex vivo  Academic Article
  • Involvement of 5-ht1a and gaba(a) receptors in the anxiolytic-like effects of cinnamomum cassia in mice  Academic Article
  • Lp-211 is a brain penetrant selective agonist for the serotonin 5-ht(7) receptor  Academic Article
  • MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport  Academic Article
  • Mechanistic insights into the Pd(BINAP)-catalyzed amination of aryl bromides: kinetic studies under synthetically relevant conditions  Academic Article
  • Mitotic checkpoint kinase Mps1 has a role in normal physiology which impacts clinical utility  Academic Article
  • Molecular determinants of selectivity and efficacy at the dopamine D3 receptor  Academic Article
  • Monitoring ligand-induced protein ordering in drug discovery  Academic Article
  • N,n-diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: A novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues  Academic Article
  • N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha(1)-adrenoceptor antagonists  Academic Article
  • Neuropeptide Y Y2R blockade in the central amygdala reduces anxiety-like behavior but not alcohol drinking in alcohol-dependent rats  Academic Article
  • New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased in vitro metabolic stability  Academic Article
  • Nitration of a peptide phytotoxin by bacterial nitric oxide synthase  Academic Article
  • Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity  Academic Article
  • Novel pharmacological probes reveal ABHD5 as a locus of lipolysis control in white and brown adipocytess  Academic Article
  • Performance of a docking/molecular dynamics protocol for virtual screening of nutlin-class inhibitors of Mdmx  Academic Article
  • Peripheral reduction of beta-amyloid is sufficient to reduce brain beta-amyloid: Implications for alzheimer's disease  Academic Article
  • Pharmacologic repression of retinoic acid receptor-related orphan nuclear receptor gamma is therapeutic in the collagen-induced arthritis experimental model  Academic Article
  • Pharmacology and antitussive efficacy of 4-(3-trifluoromethylpyridin2-yl)-piperazine-1-carboxylic acid (5-trifluoromethylpyridin2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs  Academic Article
  • Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element  Academic Article
  • Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1- (2,4-dimethyl-3-pyridinyl)carbonyl -4-methyl-4- 3(S)-methyl-4- 1(S)- 4-(trifluoro-methyl)phenyl ethyl -1-piperazinyl -piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist  Academic Article
  • Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: Synthesis, antiviral and Pharmacokinetic profiles of symmetrical Heteroaryl Carboxamides  Academic Article
  • Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1- (4,6-dimethyl-5-pyrimidinyl)carbonyl -4- 4-{2-methoxy-1(R)-4-(trifluo romethyl)-phenyl}ethyl-3(S)-methyl-1-piperazinyl -4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist  Academic Article
  • Platelet-mediated thrombosis and drug-eluting stents  Academic Article
  • Polycations. 18. The synthesis of polycationic lipid materials based on the diamine 1,4-diazabicyclo 2.2.2 octane  Academic Article
  • Potent inhibition of hiv-1 entry with a chemically programmed antibody aided by an efficient organocatalytic synthesis  Academic Article
  • Practical asymmetric synthesis of a potent cathepsin K inhibitor. Efficient palladium removal following Suzuki coupling  Academic Article
  • Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists  Academic Article
  • Printing proteins as microarrays for high-throughput function determination  Academic Article
  • Profiling of tyrosine phosphorylation pathways in human cells using mass spectrometry  Academic Article
  • Progress in small molecule therapeutics for the treatment of retinoblastoma  Academic Article
  • RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist  Academic Article
  • Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform  Academic Article
  • Role of alpha(2)-adrenoceptors in electrical field stimulation-induced contraction of pig nasal mucosa and pharmacologic characterization of a novel alpha(2C)-adrenoceptor agonist  Academic Article
  • Role of protease activated receptor 1 and 2 signaling in hypoxia-induced angiogenesis  Academic Article
  • Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A(2)  Academic Article
  • Selective mmp-inhibition with ro 28-2653 in acute experimental stroke - a magnetic resonance imaging efficacy study  Academic Article
  • Serotonin 2c receptor agonists improve type 2 diabetes via melanocortin-4 receptor signaling pathways  Academic Article
  • Serotonin(1B) receptor stimulation enhances cocaine reinforcement  Academic Article
  • Serotonin(1B) receptor stimulation enhances dopamine mediated reinforcement  Academic Article
  • Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept  Academic Article
  • Small molecule inhibitors of the CCR2b receptor. Part 1: Discovery and optimization of homopiperazine derivatives  Academic Article
  • Small molecule modulation of the human chromatid decatenation checkpoint  Academic Article
  • Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs  Academic Article
  • Structural insights into the conformational selectivity of STI-571 and related kinase inhibitors  Academic Article
  • Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II  Academic Article
  • Suppression of host p53 is critical for Plasmodium liver-stage infection  Academic Article
  • Synthesis and biological activities of phenyl piperazine-based peptidomimetic growth hormone secretagogues  Academic Article
  • Synthesis and characterization of new piperazine-type inhibitors for mitochondrial nadh-ubiquinone oxidoreductase (complex i)  Academic Article
  • Synthesis and sar of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors  Academic Article
  • Synthesis of alpha-helix mimetics with four side-chains  Academic Article
  • Synthesis of libraries of peptidomimetic compounds containing a 2-oxopiperazine unit in the main chain  Academic Article
  • Synthetic lethality in malignant pleural mesothelioma with PARP1 inhibition  Academic Article
  • Systematic identification of genomic markers of drug sensitivity in cancer cells  Academic Article
  • The 5-HT(7) receptor as a mediator and modulator of antidepressant-like behavior  Academic Article
  • The New Zealand black mouse as a model for the development and progression of chronic lymphocytic leukemia  Academic Article
  • The cell cycle-dependent nuclear import of v-jun is regulated by phosphorylation of a serine adjacent to the nuclear localization signal  Academic Article
  • The differential influence of protein-kinase inhibitors on retinal arbor morphology and eye-specific stripes in the frog retinotectal system  Academic Article
  • The dopamine d3 receptor partial agonist cjb090 and antagonist pg01037 decrease progressive ratio responding for methamphetamine in rats with extended-access  Academic Article
  • The role of 5-ht(1a) receptors in mediating the anxiogenic effects of nicotine following lateral septal administration  Academic Article
  • The sigma-receptor antagonist BD-1063 decreases ethanol intake and reinforcement in animal models of excessive drinking  Academic Article
  • Time-dependent involvement of cAMP and cGMP in consolidation of object memory: Studies using selective phosphodiesterase type 2, 4 and 5 inhibitors  Academic Article
  • Total synthesis of epicoccin G  Academic Article
  • Toward understanding the structural basis of partial agonism at the dopamine D-3 receptor  Academic Article
  • Versatile Pd(OTf)2 x 2 H2O-catalyzed ortho-fluorination using NMP as a promoter  Academic Article
  • Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration  Academic Article

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