ArticleJournal of medicinal chemistry2009
Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 29 citations in OpenAlex.
- Nonpeptidic Z360-Analogs Tagged with Trivalent Radiometals as Anti-CCKPharmaceutics · 2022Article
- [Molecular pharmaceutics · 2020Article
- Cholecystokinin-2 Receptor Targeting with Radiolabeled Peptides: Current Status and Future Directions.Current medicinal chemistry · 2020Review
- Targeting cholecystokinin-2 receptor for pancreatic cancer chemoprevention.Molecular carcinogenesis · 2019Article
- Cholecystokinin-induced satiety, a key gut servomechanism that is affected by the membrane microenvironment of this receptor.International journal of obesity supplements · 2016Review
- Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.Journal of medicinal chemistry · 2015Article
- Impact of ursodeoxycholic acid on a CCK1R cholesterol-binding site may contribute to its positive effects in digestive function.American journal of physiology. Gastrointestinal and liver physiology · 2015Article
- Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.Bioorganic & medicinal chemistry letters · 2015Article
- Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding.Molecular pharmacology · 2015Article
- A type 1 cholecystokinin receptor mutant that mimics the dysfunction observed for wild type receptor in a high cholesterol environment.The Journal of biological chemistry · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor.The Journal of biological chemistry · 2013Article
- Gastrin receptor pharmacology.Current gastroenterology reports · 2012Article
- Preclinical evaluation of radiolabeled DOTA-derivatized cyclic minigastrin analogs for targeting cholecystokinin receptor expressing malignancies.Molecular imaging and biology · 2012Article
- Molecular basis for binding and subtype selectivity of 1,4-benzodiazepine antagonist ligands of the cholecystokinin receptor.The Journal of biological chemistry · 2012Article
- Fluorescence polarization screening for allosteric small molecule ligands of the cholecystokinin receptor.Assay and drug development technologies · 2011Article
- Modulation of cell surface expression of nonactivated cholecystokinin receptors using bivalent ligand-induced internalization.Journal of medicinal chemistry · 2010Article
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
Radiolabeled antagonists of specific peptide receptors identify a higher number of receptor binding sites than agonists and may thus be preferable for in vivo tumor targeting. In this study, two novel radioiodinated 1,4-benzodiazepines, (S)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea (9) and (R)-1-(3-iodophenyl)-3-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea (7), were developed. They were characterized in vitro as high affinity selective antagonists at cholecystokinin types 1 and 2 (CCK(1) and CCK(2)) receptors using receptor binding, calcium mobilization, and internalization studies. Their binding to human tumor tissues was assessed with in vitro receptor autoradiography and compared with an established peptidic CCK agonist radioligand. The (125)I-labeled CCK(1) receptor-selective compound 9 often revealed a substantially higher amount of CCK(1) receptor binding sites in tumors than the agonist (125)I-CCK. Conversely, the radioiodinated CCK(2) receptor-selective compound 7 showed generally weaker tumor binding than (125)I-CCK. In conclusion, compound 9 is an excellent radioiodinated nonpeptidic antagonist ligand for direct and selective labeling of CCK(1) receptors in vitro. Moreover, it represents a suitable candidate to test antagonist binding to CCK(1) receptor-expressing tumors in vivo.
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