
Bioorganic and Medicinal Chemistry Letters p. 1995 - 1998 (1997)
Update date:2022-08-03
Topics:
Boyfield, Izzy
Coldwell, Martyn C.
Hadley, Michael S.
Johnson, Christopher N.
Riley, Graham J.
Scott, Emma E.
Stacey, Rachel
Stemp, Geoffrey
Thewlis, Kevin M.
A novel series of N-[4-(4-Phenylbenzoylamino)butyl]-1,2,3,4-tetrahydro-2-naphthylamines with high affinity and selectivity for the dopamine D3 receptor has been prepared. The 5-cyclopropylmethyloxy 3j, methanesulfonyloxy 3k and trifluoromethanesulfonyloxy 3l derivatives represent some of the highest affinity (pKi's 8.6-8.9) and most selective (200-320-fold) dopamine D3 receptor antagonists reported to date.
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Doi:10.1039/CT8875100040
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(2018)