Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.

Article Details

Citation

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
FluoxetineSodium-dependent serotonin transporterKi (nM)2.2N/AN/ADetails