Title : Synthesis of 3,7-disubstituted imipramines by palladium-catalysed amination/cyclisation and evaluation of their inhibition of monoamine transporters.

Pub. Date : 2011 Sep 12

PMID : 21853482






4 Functional Relationships(s)
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1 This novel TCA also exhibits an increased selectivity (relative to imipramine) in binding to hSERT versus the human norepinephrine transporter (hNET). Imipramine solute carrier family 6 member 4 Homo sapiens
2 Even higher selectivity could be obtained with 3,7-dihydroxymethyl imipramine, which was found to be 167-fold more selective for hSERT over hNET, representative of a 120-fold gain in selectivity relative to the parent imipramine. Imipramine solute carrier family 6 member 4 Homo sapiens
3 These results further validate our previous model for the binding of imipramine and high-affinity analogues of imipramine to the central binding site of hSERT. Imipramine solute carrier family 6 member 4 Homo sapiens
4 These results further validate our previous model for the binding of imipramine and high-affinity analogues of imipramine to the central binding site of hSERT. Imipramine solute carrier family 6 member 4 Homo sapiens