Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.
A novel series of 5,6,7,8-tetrahydroquinazolines, 4,5,6,7-tetrahydroindazoles and 4,5,6,7-tetrahydrobenzothiazoles has been prepared, having high affinity and selectivity for the dopamine D3 receptor. The 4-methoxy-5,6,7,8-tetrahydroquinazoline 6i and 2-amino-4,5,6,7-tetrahydrobenzothiazole 8 proved to be agonists with among the highest D3 receptor affinities and selectivities reported to date.
Avenell
K Y
KY
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
Boyfield
I
I
Hadley
M S
MS
Johnson
C N
CN
Nash
D J
DJ
Riley
G J
GJ
Stemp
G
G
D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D050637:Receptors, Dopamine D3; D013764:Tetrahydronaphthalenes / Q000737:chemistry* / Q000378:metabolism
D006571:Heterocyclic Compounds; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; D013764:Tetrahydronaphthalenes; C006561:2-aminotetralin