Abstract
The structure-activity relationship studies on 2-quinolinecarboxamide peripheral benzodiazepine receptor (PBR) ligands have been refined with the aim of using these ligands as carriers of radionuclides and boron atoms. Some new ligands show enhanced affinity and steroidogenic activity with respect to reference compound 1 and are interesting candidates for radiolabeling and PET studies. Moreover, carborane derivative 3q, representing the first example of PBR ligand bearing a carborane cage, can be useful to explore an alternative mechanism in BNCT.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology
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Animals
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Boranes / chemical synthesis*
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Boranes / chemistry
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Boranes / pharmacology
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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In Vitro Techniques
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Ligands
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Pregnanolone / biosynthesis
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Pregnenolone / biosynthesis
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Progesterone / biosynthesis
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology
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Radioligand Assay
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry
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Radiopharmaceuticals / pharmacology
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Rats
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Receptors, GABA-A / drug effects*
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Structure-Activity Relationship
Substances
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Amides
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Boranes
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Ligands
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Quinolines
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Radiopharmaceuticals
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Receptors, GABA-A
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Progesterone
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Pregnenolone
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Pregnanolone