117 articles for thisTarget
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Synthesis and biological activity of some partially modified retro-inverso analogues of cholecystokinin.
Centre De Pharmacologie-Endocrinologie (Montpellier, France)
Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines.
Merck Sharp & Dohme Research Laboratories
Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds.
TBA
Cholecystokinin antagonists. Synthesis of asperlicin analogues with improved potency and water solubility.
TBA
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.
Mayo Clinic
Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.
Mayo Clinic
Development of a time-resolved fluorescence probe for evaluation of competitive binding to the cholecystokinin 2 receptor.
University Of Arizona
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
Glaxo Wellcome Research And Development
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist"trigger".
Glaxo Wellcome
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
Glaxo Wellcome Research And Development
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
Glaxo Research Institute
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: tuning of receptor selectivity and in vivo efficacy.
Johnson & Johnson Pharmaceutical Research And Development
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Johnson & Johnson Pharmaceutical Research And Development
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.
Mayo Clinic
Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.
James Black Foundation
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Glaxo Wellcome Research And Development
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
Glaxo Research Institute
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Design and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.
University Of Arizona
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S Of Maine
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
University Of Arizona
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
Instituto De Qu£Mica M£Dica (Csic)
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
University Of Arizona
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
Merck Research Laboratories
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
University Of Paris
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.
University Of Paris
The use of topographical constraints in receptor mapping: investigation of the topographical requirements of the tryptophan 30 residue for receptor binding of Asp-Tyr-D-Phe-Gly-Trp-(N-Me)Nle-Asp-Phe-NH2 (SNF 9007), a cholecystokinin (26-33) analogue that binds to both CCK-B and delta-opioid recepto
University Of Arizona
Structure-antigastrin activity relationships of new spiroglumide amido acid derivatives.
Rotta Research Laboratorium
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.
Merck Sharp And Dohme Research Laboratories
Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity.
Abbott Laboratories
Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents.
National Cancer Institute-Frederick
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
Abbott Laboratories
CCK-A-selective tetrapeptides containing lys(N epsilon)-amide residues: favorable in vivo and in vitro effects of N-methylation at the aspartyl residue.
Abbott Laboratories
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Merck Research Laboratories
CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.
University Of Paris
Development of potent and selective CCK-A receptor agonists from Boc-CCK-4: tetrapeptides containing Lys(N epsilon)-amide residues.
Abbott Laboratories
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
Rotta Research Laboratorium
Novel glutamic acid derived cholecystokinin receptor ligands.
Merck Sharp & Dohme Research Laboratories
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
Abbott Laboratories
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.
Merck Sharp & Dohme Research Laboratories
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.
Merck Sharp & Dohme Research Laboratories
Conversion of acyclic nonpeptide CCK antagonists into CCK agonists
Glaxo Wellcome Research And Development
Synthesis of novel iodinated radioligands with high affinity and selectivity for CCK-B/gastrin receptors
TBA
Synthesis of a potent and selective non-peptide CCK-B/gastrin receptor antagonist tritiated ligand.
TBA
New anthranilic acid based antagonists with high affinity and selectivity for the human cholecystokinin receptor 1 (hCCK1-R).
University Of Trieste
A sucrose-derived scaffold for multimerization of bioactive peptides.
The University Of Arizona
Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor.
University Medical Centre Ljubljana
Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
Merck
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical And Public Health Institute
Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists
TBA
Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists
TBA
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
TBA
Potent, selective, water-soluble benzodiazepine-based CCKB receptor antagonists that contain lipophilic carboxylate surrogates
TBA
Diphenylpyrazolidinone and benzodiazepine cholecystokinin antagonists: A case of convergent evolution in medicinal chemistry
TBA
Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists
TBA
Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics
TBA
Tryptophan-norleucine 1,5-disubstituted tetrazoles as cis peptide bond mimics: Investigation of the bioactive conformation of a potent and selective peptide for the cholecystokinin-B receptor
TBA
L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCKB/gastrin receptor
TBA
1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists
TBA
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands.
University Of Minnesota
Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
Merck Research Laboratories
Recent natural products based drug development: a pharmaceutical industry perspective.
Bristol-Myers Squibb Pharmaceutical Research Institute
Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
University Of Arizona
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.
Johnson And Johnson Pharmaceutical Research And Development
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Combination of molecular modeling, site-directed mutagenesis, and SAR studies to delineate the binding site of pyridopyrimidine antagonists on the human CCK1 receptor.
Instituto De QuíMica MéDica (Csic)
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
University Of Paris
Relationship between dihedral angles of N1 and C9 substituents in 1,4-benzodiazepines and dual cholecystokinin-A and -B antagonistic activities.
Fujisawa Pharmaceutical
Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.
Parke-Davis Pharmaceutical Research
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.
Merck Research Laboratories
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.
Merck Sharp & Dohme Research Laboratories
Minor structural differences in Boc-CCK-4 derivatives dictate affinity and selectivity for CCK-A and CCK-B receptors.
Abbott Laboratories
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Universitá
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Neuroscience Research Centre
Cholecystokinin peptidomimetics as selective CCK-B antagonists: design, synthesis, and in vitro and in vivo biochemical properties.
University Of Paris
Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.
Merck Research Laboratories
Ac-[3- and 4-alkylthioproline31]-CCK4 analogs: synthesis and implications for the CCK-B receptor-bound conformation.
Washington University
Synthesis and biological evaluation of cholecystokinin analogs in which the Asp-Phe-NH2 moiety has been replaced by a 3-amino-7-phenylheptanoic acid or a 3-amino-6-(phenyloxy)hexanoic acid.
Ep Cnrs 51
Synthesis and biological activity of partially modified retro-inverso pseudopeptide derivatives of the C-terminal tetrapeptide of gastrin.
TBA
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.
Merck Sharp & Dohme Research Laboratories
Synthesis of gastrin antagonists, analogues of the C-terminal tetrapeptide of gastrin, by introduction of a beta-homo residue.
Centre De Pharmacologie-Endocrinologie (Montpellier, France)
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
University Of Paris
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
Merck Sharp & Dohme Research Laboratories
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Abbott Laboratories
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
Abbott Laboratories
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
Abbott Laboratories
Boc-Trp-Orn(Z)-Asp-NH2 and derivatives: a new family of CCK antagonists.
University Of Paris
Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.
Abbott Laboratories
N-methylated analogs of Ac[Nle28,31]CCK(26-33): synthesis, activity, and receptor selectivity.
Hadassah-University Hospital
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.
Yogi Vemana University