PMID

Data

Article Title

Organization

Spirotetronate polyketides as leads in drug discovery.

University of California San Diego

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

Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.

James Black Foundation

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)

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.

Instituto De Qu£Mica M£Dica (Csic)

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1)receptor antagonists: structure-activity relationship studies on the substituent at N2-position.

Instituto De Qu£Mica M£Dica (Csic)

beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.

Instituto De Qu£Mica M£Dica (Csic)

CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.

Astrazeneca R&D Boston

5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.

Insituto De Qu�Mica M�Dica (Csic)

Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.

University of Paris

Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.

Rochester

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

Peptide-linked 1,3-dialkyl-3-acyltriazenes: gastrin receptor directed antineoplastic alkylating agents.

National Cancer Institute-Frederick

CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.

University of Paris

Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.

Rotta Research Laboratorium

Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.

University of Paris

 

Pseudopeptide CCK-4 analogues incorporating the [CH(CN)NH] peptide bond surrogate

TBA

 

Identification and biological activity of novel peptidomimetic gastrin/CCK-B receptor agonists

TBA

Highly improved metabolic stability and pharmacokinetics of indium-111-DOTA-gastrin conjugates for targeting of the gastrin receptor.

University Medical Centre Ljubljana

 

CCK-4 restricted analogues containing a 3-oxoindolizidine skeleton

TBA

 

Synthesis and biological activity of 5-heteroaryl benzodiazepines: analogues of YM022

TBA

 

Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022

TBA

 

On the significance of the C-terminal primary amide in cholecystokinin

TBA

 

Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics

TBA

Conformationally constrained CCK4 analogues incorporating IBTM and BTD beta-turn mimetics.

Instituto De QuíMica MéDica (Csic)

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)

Stabilization Strategies for Linear Minigastrin Analogues: Further Improvements

Medical University of Innsbruck

Effects of the incorporation of IBTM beta-turn mimetics into the dipeptoid CCK(1) receptor agonist PD 170292.

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

Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.

University of Paris

Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.

Instituto De QuíMica MéDica (Csic)

(3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.

Ferring Research Institute

Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.

Mayo Foundation

Cholecystokinin peptidomimetics as selective CCK-B antagonists: design, synthesis, and in vitro and in vivo biochemical properties.

University of Paris

Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar

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 SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.

Glaxo Wellcome Medicines Research Centre

Carboxylic acids and tetrazoles as isosteric replacements for sulfate in cholecystokinin analogues.

Roche Research Center

Analogs of CCK incorporating conformationally constrained replacements for Asp32.

Roche Research Center

Analogs of Ac-CCK-7 incorporating dipeptide mimics in place of Met28-Gly29.

Roche Research Center

N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties.

Pudue Pharma Discovery Research

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Janssen Research Foundation

ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.

Abbott Laboratories

Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.

Janssen Research Foundation

Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist.

University of Occupational and Environmental Health

GR113808: a novel, selective antagonist with high affinity at the 5-HT4 receptor.

Glaxo Group Research

Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo.

Merck Sharp and Dohme Research Laboratories

Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.

Yamanouchi Pharmaceutical

Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors.

Sanofi Recherche

Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide.

Fujisawa Pharmaceutical

A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260.

Merck Sharp & Dohme Research Laboratories

Neurochemical profile of eltoprazine.

Duphar

Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.

Center For Bio-Pharmaceutical Sciences