Journal ArticleDOI
Development of 1,4-Benzodiazepine Cholecystokinin Type B Antagonists.
Mark G. Bock,Robert M. DiPardo,B. E. Evans,Kenneth E. Rittle,W. L. Whitter,V. M. Garsky,Kevin F. Gilbert,James L. Leighton,K. L. Carson,E. C. Mellin,D. F. Veber,R. S. L. Chang,Victor J. Lotti,Stephen B. Freedman,A. J. Smith,Shil Patel,P. S. Anderson,Roger M. Freidinger +17 more
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This article is published in ChemInform.The article was published on 1994-06-28. It has received 6 citations till now.read more
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Journal ArticleDOI
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
Antonella Ursini,Anna M. Capelli,Robin A. E. Carr,Paolo Cassarà,Mauro Corsi,O. Curcuruto,Giovanni Curotto,Michele Dal Cin,Silvia Davalli,Daniele Donati,Aldo Feriani,Harry Finch,Gabriella Finizia,Giovanni Gaviraghi,Marc Marien,Giorgio Pentassuglia,Stefano Polinelli,E. Ratti,Aldo Reggiani,Giorgio Tarzia,Giovanna Tedesco,Maria Elvira Tranquillini,and David G. Trist,Frank Th.M. van Amsterdam +23 more
TL;DR: A series of 5-phenyl-3-ureidobenzodiazepine-2,4-diones was synthesized and evaluated as cholecystokinin-B (CCK-B) receptor antagonists and the introduction of bulky substituents such as adamantylmethyl at N-1 resulted in the lead compound GV150013.
Journal ArticleDOI
Induced association of mu opioid (MOP) and type 2 cholecystokinin (CCK2) receptors by novel bivalent ligands
Yaguo Zheng,Eyup Akgün,Kaleeckal G. Harikumar,Jessika Hopson,Michael D. Powers,Mary M. Lunzer,Laurence J. Miller,Philip S. Portoghese +7 more
TL;DR: These studies demonstrate for the first time that an appropriately designed bivalent ligand is capable of inducing association of G-protein-coupled receptors.
Journal ArticleDOI
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.
Eyup Akgün,Meike Körner,Meike Körner,Fan Gao,Kaleeckal G. Harikumar,Beatrice Waser,Jean Claude Reubi,Philip S. Portoghese,Laurence J. Miller +8 more
TL;DR: Radioiodinated 1,4-benzodiazepines compound 9 is an excellent radioiodinated nonpeptidic antagonist ligand for direct and selective labeling of CCK (1) receptors in vitro and represents a suitable candidate to test antagonist binding to CCK(1) receptor-expressing tumors in vivo.
Journal ArticleDOI
Future Prospects for the Pharmacological Treatment of Anxiety
TL;DR: Findings are improving the prospect of alternatives to the benzodiazepines in the treatment of anxiety disorders, and Benzodiazepine receptor partial agonists have been developed that have more anxio-selective profiles than those of full agonists.
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Journal ArticleDOI
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.
Mark G. Bock,Robert M. DiPardo,Ben E. Evans,Kenneth E. Rittle,Willie L. Whitter,Victor M. Garsky,Kevin F. Gilbert,James L. Leighton,Kenneth L. Carson +8 more
TL;DR: Details of the ability to modulate the receptor interactions of these benzodiazepines by appropriate structure modifications are discussed which imply the possibility of further refining the CCK-B receptor affinity and selectivity of this class of compounds.
Related Papers (5)
Discovery of 1,5‐Benzodiazepines with Peripheral Cholecystokinin (CCK‐ A) Receptor Agonist Activity (II): Optimization of the C3 Amino Substituent.
Gavin C. Hirst,Christopher Joseph Aquino,L.S. Birkemo,Dallas K. Croom,Milana Dezube,R. W. Jun. Dougherty,Gregory N. Ervin,Mary K. Grizzle,Brad R. Henke,Michael K. James,Michael F. Johnson,Tanya M. Momtahen,Kennedy L. Queen,Ronald George Sherrill,Szewczyk Jerzy Ryszard,Timothy M. Willson,Elizabeth E. Sugg +16 more