1745-07-9, Name is 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline, belongs to tetrahydroisoquinoline compound, is a common compound. Product Details of 1745-07-9In an article, once mentioned the new application about 1745-07-9.
The sigma-2 (sigma2) receptor has been suggested to be a promising target for pharmacological interventions to curb tumor progression. Development of sigma2-specific ligands, however, has been hindered by lack of understanding of molecular determinants that underlie selective ligand-sigma2 interactions. Here we have explored effects of electron donating and withdrawing groups on ligand selectivity for the sigma2 versus sigma1 receptor using new benzamide-isoquinoline derivatives. The electron-donating methoxy group increased but the electron-withdrawing nitro group decreased sigma2 affinity. In particular, an extra methoxy added to the para-position (5e) of the benzamide phenyl ring of 5f dramatically improved (631 fold) the sigma2 selectivity relative to the sigma1 receptor. This para-position provided a sensitive site for effective manipulation of the sigma receptor subtype selectivity using either the methoxy or nitro substituent. Our study provides a useful guide for further improving the sigma2-over-sigma1 selectivity of new ligands.
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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem