D4 dopamine receptor-selective compounds from the Chinese plant Phoebe chekiangensis

Bioorganic & Medicinal Chemistry Letters
1997.0

Abstract

5-Hydroxy-indoline (1), tyramine (2), N-norarmepavine (3), and a novel glycosylated tetrahydroisoquinoline analog SCH 71450 (4) were all isolated from a methanol extract from the fruit of the Chinese plant Phoebe chekiangensis based on their activity in displacing D 4 dopaminergic receptor ligand binding. These compounds and related natural products were evaluated for D 4 receptor selectivity relative to D 2 receptor binding displacement. Compounds 1 and 4 exhibited better D 4 selectivity than standard dopaminergic antagonists including the clinically useful compound clozapine. GppNHp shifts in displacement curves indicated that compound 1 is an agonist while compound 4 is an antagonist.

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