subject area of
- 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