Abstract
A series of 2-subsdtuted N- n-propylnorapomorphine (NPA) derivatives were synthesized and compared with other DA agonists for affinity to D 1 and D 2 dopamine (DA) receptors in rat brain corpus striatum tissue. The 2-substitutents tested reduced D1 affinity similarly, but enhanced D 2 affinity in the rank order: F > OH > Br > OCH 3 > H ≥ NH 2. The extraordinarily high D 2 affinity (K i = 12 pM) and D 2 vs. D 1 selectivity (57,500) of 2-F-NPA far-exceeded that of all ot DA agonists tested, and it was about 10-times more potent than NPA in vivo.
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