Abstract
AIM
To compare the actions of tetrahydroprotoberberines (THPB) on dopamine (DA) D2 receptors in the ventral tegmental area (VTA) of rat.
METHODS
Extracellular single unit recording technique was used in i.v. gallamine-paralyzed rats.
RESULTS
Eleven THPB analogs tested completely attenuated the apomorphine (Apo, 20 micrograms.kg-1)-induced inhibition on VTA DA cell firing activity. The OH group on C2 at THPB was linked with the reversal of Apo-induced inhibition. Their reversal potencies (ED50, microgram.kg-1) for D2 receptors were: THPB-143 (5.6) > SPD (8.5) > Iso (17.0) > THP (33) > THB (48) > THPB-18 (66) > THPB-1 (179) > THPB-19 (408) > THPB-126 (510) > THPB-104 (1019) > THPB-10 (4815).
CONCLUSION
Among these 11 THPB, the 2-hydroxyl-THPB (THPB-143) showed the strongest antagonistic action on D2 receptors.
TY - JOUR
T1 - Effects of tetrahydroprotoberberines on dopamine D2 receptors in ventral tegmental area of rat.
AU - Wang,L M,
AU - Zhang,X X,
AU - Jin,G Z,
PY - 1997/3/1/pubmed
PY - 1999/3/12/medline
PY - 1997/3/1/entrez
SP - 143
EP - 6
JF - Zhongguo yao li xue bao = Acta pharmacologica Sinica
JO - Zhongguo Yao Li Xue Bao
VL - 18
IS - 2
N2 - AIM: To compare the actions of tetrahydroprotoberberines (THPB) on dopamine (DA) D2 receptors in the ventral tegmental area (VTA) of rat. METHODS: Extracellular single unit recording technique was used in i.v. gallamine-paralyzed rats. RESULTS: Eleven THPB analogs tested completely attenuated the apomorphine (Apo, 20 micrograms.kg-1)-induced inhibition on VTA DA cell firing activity. The OH group on C2 at THPB was linked with the reversal of Apo-induced inhibition. Their reversal potencies (ED50, microgram.kg-1) for D2 receptors were: THPB-143 (5.6) > SPD (8.5) > Iso (17.0) > THP (33) > THB (48) > THPB-18 (66) > THPB-1 (179) > THPB-19 (408) > THPB-126 (510) > THPB-104 (1019) > THPB-10 (4815). CONCLUSION: Among these 11 THPB, the 2-hydroxyl-THPB (THPB-143) showed the strongest antagonistic action on D2 receptors.
SN - 0253-9756
UR - https://www.unboundmedicine.com/medline/citation/10072967/Effects_of_tetrahydroprotoberberines_on_dopamine_D2_receptors_in_ventral_tegmental_area_of_rat_
L2 - http://www.chinaphar.com/1671-4083/18/143.pdf
DB - PRIME
DP - Unbound Medicine
ER -