PubRank

Peter Gmeiner

Author PubWeight™ 86.91‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Structure and function of an irreversible agonist-β(2) adrenoceptor complex. Nature 2011 5.35
2 Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature 2013 2.49
3 Quinpramine is a novel compound effective in ameliorating brain autoimmune disease. Exp Neurol 2008 1.44
4 Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists. J Med Chem 2002 1.44
5 The structural evolution of dopamine D3 receptor ligands: structure-activity relationships and selected neuropharmacological aspects. Pharmacol Ther 2006 1.33
6 Dopamine D2, D3, and D4 selective phenylpiperazines as molecular probes to explore the origins of subtype specific receptor binding. J Med Chem 2009 1.18
7 Tricyclic antidepressants, quinacrine and a novel, synthetic chimera thereof clear prions by destabilizing detergent-resistant membrane compartments. J Neurochem 2006 1.13
8 Recent advances in the search for D3- and D4-selective drugs: probes, models and candidates. Trends Pharmacol Sci 2011 1.10
9 Rational Molecular Design and EPC Synthesis of a Type VI beta-Turn Inducing Peptide Mimetic This work was supported by the BMBF and the Fonds der Chemischen Industrie. EPC=enantiomerically pure compound. Angew Chem Int Ed Engl 2001 1.06
10 Dopamine D2 and D3 receptors in human putamen, caudate nucleus, and globus pallidus. Synapse 2006 1.05
11 Labeling and glycosylation of peptides using click chemistry: a general approach to (18)F-glycopeptides as effective imaging probes for positron emission tomography. Angew Chem Int Ed Engl 2010 1.03
12 Evaluation of lactam-bridged neurotensin analogues adjusting psi(Pro10) close to the experimentally derived bioactive conformation of NT(8-13). J Med Chem 2004 1.01
13 Chirospecific synthesis of spirocyclic beta-lactams and their characterization as potent type II beta-turn inducing peptide mimetics. J Org Chem 2006 1.01
14 Histidine 6.55 is a major determinant of ligand-biased signaling in dopamine D2L receptor. Mol Pharmacol 2010 0.98
15 Structure-based design of Tet repressor to optimize a new inducer specificity. Biochemistry 2004 0.97
16 Argyreia nervosa (Burm. f.): receptor profiling of lysergic acid amide and other potential psychedelic LSD-like compounds by computational and binding assay approaches. J Ethnopharmacol 2013 0.96
17 Fancy bioisosteres: novel paracyclophane derivatives as super-affinity dopamine D3 receptor antagonists. J Med Chem 2006 0.96
18 A chimeric ligand approach leading to potent antiprion active acridine derivatives: design, synthesis, and biological investigations. J Med Chem 2006 0.96
19 Functionally selective dopamine D₂, D₃ receptor partial agonists. J Med Chem 2014 0.93
20 A gene regulation system with four distinct expression levels. J Gene Med 2006 0.93
21 Class A G-protein-coupled receptor (GPCR) dimers and bivalent ligands. J Med Chem 2013 0.92
22 Certain 1,4-disubstituted aromatic piperidines and piperazines with extreme selectivity for the dopamine D4 receptor interact with a common receptor microdomain. Mol Pharmacol 2004 0.92
23 Modeling the similarity and divergence of dopamine D2-like receptors and identification of validated ligand-receptor complexes. J Med Chem 2005 0.90
24 Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1. Bioorg Med Chem 2008 0.89
25 Bivalent dopamine D2 receptor ligands: synthesis and binding properties. J Med Chem 2011 0.89
26 CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists. J Med Chem 2005 0.88
27 In vitro affinities of various halogenated benzamide derivatives as potential radioligands for non-invasive quantification of D(2)-like dopamine receptors. Bioorg Med Chem 2007 0.88
28 SCRF-DFT and NMR comparison of tetracycline and 5a,6-anhydrotetracycline in solution. J Phys Chem B 2006 0.88
29 Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands. J Med Chem 2007 0.88
30 Functionally selective dopamine D2/D3 receptor agonists comprising an enyne moiety. J Med Chem 2013 0.87
31 Muscarinic receptors as model targets and antitargets for structure-based ligand discovery. Mol Pharmacol 2013 0.87
32 Active-state models of ternary GPCR complexes: determinants of selective receptor-G-protein coupling. PLoS One 2013 0.87
33 Dopamine D3 receptor ligands: recent advances in the control of subtype selectivity and intrinsic activity. Biochim Biophys Acta 2006 0.87
34 18F-Labeled FAUC 346 and BP 897 derivatives as subtype-selective potential PET radioligands for the dopamine D3 receptor. ChemMedChem 2008 0.87
35 Highly potent 5-aminotetrahydropyrazolopyridines: enantioselective dopamine D3 receptor binding, functional selectivity, and analysis of receptor-ligand interactions. J Med Chem 2011 0.86
36 3,4,6-Tri-O-acetyl-2-deoxy-2-[18F]fluoroglucopyranosyl phenylthiosulfonate: a thiol-reactive agent for the chemoselective 18F-glycosylation of peptides. Bioconjug Chem 2007 0.86
37 Functional characterization of a partial loss-of-function mutation of the epithelial sodium channel (ENaC) associated with atypical cystic fibrosis. Cell Physiol Biochem 2009 0.86
38 Molecular dynamics simulations of the effect of the G-protein and diffusible ligands on the β2-adrenergic receptor. J Mol Biol 2011 0.85
39 PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain. Eur J Neurosci 2006 0.85
40 Pharmacophore-guided drug discovery investigations leading to bioactive 5-aminotetrahydropyrazolopyridines. Implications for the binding mode of heterocyclic dopamine D3 receptor agonists. J Med Chem 2005 0.84
41 Discovery of highly potent and neurotensin receptor 2 selective neurotensin mimetics. J Med Chem 2011 0.84
42 Development of a metabolically stable neurotensin receptor 2 (NTS2) ligand. ChemMedChem 2012 0.84
43 Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. Bioorg Med Chem Lett 2008 0.84
44 2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist. J Med Chem 2006 0.83
45 Click linker: efficient and high-yielding synthesis of a new family of SPOS resins by 1,3-dipolar cycloaddition. Org Lett 2003 0.82
46 Fancy bioisosteres: synthesis, SAR, and pharmacological investigations of novel nonaromatic dopamine D3 receptor ligands. Bioorg Med Chem 2005 0.82
47 Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors. J Med Chem 2013 0.82
48 Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype. Bioorg Med Chem Lett 2004 0.82
49 Click chemistry on solid phase: parallel synthesis of N-benzyltriazole carboxamides as super-potent G-protein coupled receptor ligands. J Comb Chem 2006 0.82
50 Syntheses, receptor bindings, in vitro and in vivo stabilities and biodistributions of DOTA-neurotensin(8-13) derivatives containing β-amino acid residues - a lesson about the importance of animal experiments. Chem Biodivers 2013 0.82
51 Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles. J Med Chem 2005 0.82
52 Dopamine D2-like receptor agonists induce penile erection in male rats: differential role of D2, D3 and D4 receptors in the paraventricular nucleus of the hypothalamus. Behav Brain Res 2011 0.81
53 Subtype selective tetracycline agonists and their application for a two-stage regulatory system. Chembiochem 2006 0.81
54 Development of a bivalent dopamine D₂ receptor agonist. J Med Chem 2011 0.81
55 Bivalent molecular probes for dopamine D2-like receptors. Bioorg Med Chem 2011 0.81
56 Biotransformation of 21-O-acetyl-deoxycorticosterone by cell suspension cultures of Digitalis lanata (strain W.1.4). Steroids 2012 0.80
57 Fancy bioisosteres: synthesis and dopaminergic properties of the endiyne FAUC 88 as a novel non-aromatic D3 agonist. Bioorg Med Chem 2005 0.80
58 Novel D3 selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies. J Med Chem 2008 0.80
59 Cross-receptor interactions between dopamine D2L and neurotensin NTS1 receptors modulate binding affinities of dopaminergics. ACS Chem Neurosci 2011 0.80
60 Engineering a GPCR-ligand pair that simulates the activation of D(2L) by Dopamine. ACS Chem Neurosci 2009 0.79
61 Indoloparacyclophanes: Synthesis and Dopamine Receptor Binding of a Novel Arylbioisostere This work was supported by the Fonds der Chemischen Industrie. Angew Chem Int Ed Engl 2001 0.79
62 FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia. Psychopharmacology (Berl) 2004 0.79
63 Analogues of FAUC 73 revealing new insights into the structural requirements of nonaromatic dopamine D3 receptor agonists. Bioorg Med Chem 2004 0.79
64 The pH probe CypHer™5E is effectively quenched by FM dyes. J Fluoresc 2013 0.79
65 A new D₂ dopamine receptor agonist allosterically modulates A(2A) adenosine receptor signalling by interacting with the A(2A)/D₂ receptor heteromer. Cell Signal 2011 0.78
66 On the terminal homologation of physiologically active peptides as a means of increasing stability in human serum--neurotensin, opiorphin, B27-KK10 epitope, NPY. Chem Biodivers 2011 0.78
67 1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands. J Med Chem 2009 0.78
68 Bioisosteric replacement leading to biologically active [2.2]paracyclophanes with altered binding profiles for aminergic G-protein-coupled receptors. J Med Chem 2010 0.78
69 The bulky N6 substituent of cabergoline is responsible for agonism of this drug at 5-hydroxytryptamine 5-HT2A and 5-HT2B receptors and thus is a determinant of valvular heart disease. J Pharmacol Exp Ther 2011 0.78
70 Selective agonists for dopamine/neurotensin receptor heterodimers. ChemMedChem 2011 0.78
71 A highly practical RCM approach towards a molecular building kit of spirocyclic reverse turn mimics. Chemistry 2006 0.78
72 2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356. Bioorg Med Chem Lett 2002 0.78
73 Diarylpropane-1,3-dione derivatives as TetR-inducing tetracycline mimetics: Synthesis and biological investigations. Chembiochem 2009 0.78
74 Characterization of the molecular fragment that is responsible for agonism of pergolide at serotonin 5-Hydroxytryptamine2B and 5-Hydroxytryptamine2A receptors. J Pharmacol Exp Ther 2007 0.78
75 Synthesis, radiofluorination, and in vitro evaluation of pyrazolo[1,5-a]pyridine-based dopamine D4 receptor ligands: discovery of an inverse agonist radioligand for PET. J Med Chem 2008 0.77
76 Bicyclic melatonin receptor agonists containing a ring-junction nitrogen: Synthesis, biological evaluation, and molecular modeling of the putative bioactive conformation. Bioorg Med Chem 2005 0.77
77 The therapeutically anti-prion active antibody-fragment scFv-W226: paramagnetic relaxation-enhanced NMR spectroscopy aided structure elucidation of the paratope-epitope interface. J Biomol Struct Dyn 2010 0.77
78 Impact of the proline residue on ligand binding of neurotensin receptor 2 (NTS2)-selective peptide-peptoid hybrids. ChemMedChem 2013 0.77
79 Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents. Bioorg Med Chem Lett 2005 0.77
80 Fast and efficient (18) F-labeling by [(18) f]fluorophenylazocarboxylic esters. Chemistry 2013 0.77
81 Dopamine agonist-induced penile erection and yawning: a comparative study in outbred Roman high- and low-avoidance rats. Pharmacol Biochem Behav 2013 0.77
82 Novel azulene derivatives for the treatment of erectile dysfunction. Bioorg Med Chem Lett 2012 0.77
83 Molecular building kit of fused-proline-derived peptide mimetics allowing specific adjustment of the dihedral Psi angle. J Org Chem 2007 0.77
84 A series of 18F-labelled pyridinylphenyl amides as subtype-selective radioligands for the dopamine D3 receptor. ChemMedChem 2010 0.76
85 Attenuation of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) neurotoxicity by the novel selective dopamine D3-receptor partial agonist FAUC 329 predominantly in the nucleus accumbens of mice. Biochem Pharmacol 2003 0.76
86 Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists. J Med Chem 2010 0.76
87 Proline derived spirobarbiturates as highly effective beta-turn mimetics incorporating polar and functionalizable constraint elements. J Org Chem 2008 0.76
88 The azulene framework as a novel arene bioisostere: design of potent dopamine D4 receptor ligands inducing penile erection. ChemMedChem 2009 0.76
89 A general approach to dehydro-Freidinger lactams: ex-chiral pool synthesis and spectroscopic evaluation as potential reverse turn inducers. J Org Chem 2003 0.76
90 Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand. Org Biomol Chem 2011 0.76
91 Aromatic ring functionalization of benzolactam derivatives: new potent dopamine D3 receptor ligands. Bioorg Med Chem Lett 2010 0.76
92 Evaluation of 18F-labeled benzodioxine piperazine-based dopamine D4 receptor ligands: lipophilicity as a determinate of nonspecific binding. J Med Chem 2011 0.76
93 Chirospecific and subtype selective dopamine receptor binding of heterocyclic methoxynaphthamide analogs. Arch Pharm (Weinheim) 2005 0.76
94 Parallel synthesis and biological screening of dopamine receptor ligands taking advantage of a click chemistry based BAL linker. J Comb Chem 2005 0.76
95 Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers. Bioorg Med Chem Lett 2013 0.76
96 CoMFA and CoMSIA investigations of dopamine D3 receptor ligands leading to the prediction, synthesis, and evaluation of rigidized FAUC 365 analogues. Bioorg Med Chem 2006 0.76
97 Tetracycline sensing using novel doxycycline derivatives immobilized on different surface plasmon resonance biosensor surfaces. Bioanalysis 2010 0.75
98 Parallel synthesis of potent dopaminergic N-phenyltriazole carboxamides applying a novel click chemistry based phenol linker. Bioorg Med Chem 2009 0.75
99 Quinpramine ameliorates rat experimental autoimmune neuritis and redistributes MHC class II molecules. PLoS One 2011 0.75
100 Anhydrotetracycline-peptide conjugates as representatives for ligand-based transactivating systems. Bioorg Med Chem 2010 0.75
101 Structure-based design and discovery of new M2 receptor agonists. J Med Chem 2017 0.75
102 Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases. Bioorg Med Chem 2009 0.75
103 Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging. Bioorg Med Chem Lett 2014 0.75
104 Structural origins for selectivity and specificity in an engineered bacterial repressor-inducer pair. FEBS J 2009 0.75
105 Di- and trisubstituted pyrazolo[1,5-a]pyridine derivatives: synthesis, dopamine receptor binding and ligand efficacy. Bioorg Med Chem Lett 2002 0.75
106 Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid. Bioorg Med Chem Lett 2003 0.75
107 A highly efficient type I β-turn mimetic simulating an Asx-Pro-turn-like structure. Org Lett 2011 0.75
108 Click-chemistry-derived tetracycline-amino acid conjugates exhibiting exceptional potency and exclusive recognition of the reverse tet repressor. Chembiochem 2010 0.75
109 Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype. Bioorg Med Chem Lett 2006 0.75
110 Fused azaindole derivatives: molecular design, synthesis and in vitro pharmacology leading to the preferential dopamine D3 receptor agonist FAUC 725. Bioorg Med Chem Lett 2002 0.75
111 Clozapine derived 2,3-dihydro-1H-1,4- and 1,5-benzodiazepines with D4 receptor selectivity: synthesis and biological testing. Bioorg Med Chem 2004 0.75
112 A simple chemical method for synthesizing malonyl hemiesters of 21-hydroxypregnanes, potential intermediates in cardenolide biosynthesis. Steroids 2007 0.75
113 Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312. Bioorg Med Chem Lett 2003 0.75
114 Discovery of a dopamine D4 selective PET ligand candidate taking advantage of a click chemistry based REM linker. Bioorg Med Chem Lett 2008 0.75
115 Discovery of dopamine D₄ receptor antagonists with planar chirality. Bioorg Med Chem 2013 0.75
116 Phenylpiperazinylmethylindolecarboxylates and derivatives as selective D(4)-ligands. Bioorg Med Chem 2002 0.75
117 Click chemistry based solid phase supported synthesis of dopaminergic phenylacetylenes. Bioorg Med Chem 2007 0.75