Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
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Letavic MA, Keith JM, Ly KS, Barbier AJ, Boggs JD, Wilson SJ, Lord B, Lovenberg TW, Carruthers NI
Novel naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
Bioorg Med Chem Lett. 2007 May 1;17(9):2566-9. Epub 2007 Feb 4.
- PubMed ID
- 17307358 [ View in PubMed]
- Abstract
A series of novel tetrahydronaphthyridine-based histamine H(3) ligands that have serotonin reuptake transporter inhibitor activity is described. The 1,2,3,4-tetrahydro-2,6-naphthyridine scaffold is assembled via the addition of a nitrostyrene to a metalated pyridine followed by reduction and cyclization to form the naphthyridine. In vitro biological data for these novel compounds are discussed.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Fluoxetine Sodium-dependent serotonin transporter Ki (nM) 2.2 N/A N/A Details