Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
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Letavic MA, Keith JM, Jablonowski JA, Stocking EM, Gomez LA, Ly KS, Miller JM, Barbier AJ, Bonaventure P, Boggs JD, Wilson SJ, Miller KL, Lord B, McAllister HM, Tognarelli DJ, Wu J, Abad MC, Schubert C, Lovenberg TW, Carruthers NI
Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
Bioorg Med Chem Lett. 2007 Feb 15;17(4):1047-51. Epub 2006 Nov 16.
- PubMed ID
- 17127059 [ View in PubMed]
- Abstract
A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic 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