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Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor. 1999
N E Austin, and
K Y Avenell, and
I Boyfield, and
C L Branch, and
M C Coldwell, and
M S Hadley, and
P Jeffrey, and
A Johns, and
C N Johnson, and
D J Nash, and
G J Riley, and
S A Smith, and
R C Stacey, and
G Stemp, and
K M Thewlis, and
A K Vong
SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Using clearance and brain penetration studies as a screen, tetrahydroisoquinoline 3 was identified as a lead having low clearance in rats (CLb 20 ml/min/kg). Introduction of a 7-CF3SO2O- substituent into the tetrahydroisoquinoline, followed by replacement of the biphenylamido group of 3 by a 3-indolylpropenamido group gave 31, having high D3 receptor affinity (pKi 8.4) and 150 fold selectivity over the D2 receptor.
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