Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline,(R)-(+)-nor-roefractine

N Cabedo, P Protais, BK Cassels…

Index: Cabedo, Nuria; Protais, Philippe; Cassels, Bruce K.; Cortes, Diego Journal of Natural Products, 1998 , vol. 61, # 6 p. 709 - 712

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Citation Number: 35

Abstract

(R)-(+)-nor-Roefractine (1) was synthesized by the Bischler-Napieralski route, using asymmetric reduction of the 1, 2-didehydro precursor imine with sodium (S)-N-CBZ- prolinyloxyborohydride. Compound 1 was able to displace [3H]-raclopride (a D2 dopamine receptor-selective ligand) from its specific binding sites in rat striatum with selectivity vs [3H]- SCH23390 (D1 dopamine receptor-selective ligand).