Lm. Wang et al., EFFECTS OF TETRAHYDROPROTOBERBERINES ON DOPAMINE D-2 RECEPTORS IN VENTRAL TEGMENTAL AREA OF RAT, Zhongguo yaoli xuebao, 18(2), 1997, pp. 143-146
AIM: To compare the actions of tetrahydroprotoberberines (THPB) on dop
a;nine (DA) D-2 receptors in the ventral tegmental area (VTA) of rat.
METHODS: Extracellular single unit recording technique was used in iv
gallamine-paralyzed rats. RESULTS: Eleven THPB analogs tested complete
ly attenuated the apomorphine (Apo, 20 mu g . kg(-1))-induced inhibiti
on on VTA DA cell firing activity. The OH group on C-2 at THPB was lin
ked with the reversal of Apo-induced inhibition. Their reversal potenc
ies (ED(50), mu g . L(-1)) for D-2 receptors were: THPB-143 (5.6) > SP
D (8.5) > Iso (17.0) > THP (33) > THE (48) > THPB-18 (66) > THPB-1 (17
9) > THPB-19 (408) > THPI-126 (510) > THPB-104 (1019) > THPB-10 (4815)
. CONCLUSION: Among these 11 THPB, the 2-hydroxyl-THPB (THPB-143) show
ed the strongest antagonistic action on D-2 receptors.