An ethnopharmacological survey showed that home remedies prepared with
flowers and fruits of Psychotria colorata are used by Amazonian peasa
nts as pain killers. Psychopharmacological in vivo evaluation of alkal
oids obtained from leaves and flowers of this species showed a marked
dose-dependent naloxone-reversible analgesic activity, therefore sugge
sting an opioid-like pharmacological profile. This paper reports an in
hibitory effect of P. colorata flower alkaloids on [H-3]naloxone bindi
ng in rat striata as well as a decrease in adenylate cyclase basal act
ivity. The alkaloids did not affect [H-3] GMP-PNP binding. These findi
ngs provide a neurochemical basis for the opioid-like activity previou
sly detected in vivo and point to Psychotria alkaloids as a potential
source of new bioactive opiate derivatives.