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Characteristics of tetrahydroprotoberberines on dopamine D1 and D2 receptors in calf striatum.
Zhongguo Yao Li Xue Bao. 1997 May; 18(3):225-30.ZY

Abstract

AIM

To study the characteristics of tetrahydroprotoberberines (THPB) on dopamine D1 and D2 receptors and elucidate their structure-activity relationship.

METHODS

Radioligand assay in vitro with a two-site model program analysis.

RESULTS

Four THPB with two hydorxyl groups on C2 and C9 or C2 and C10 exhibited RH and RL two binding sites to D1 receptors and guanosine triphosphate regulated the RH binding site of SPD and THPB-132A in competition assay, while eleven THPB including nonhydroxy-THPB, monohydroxy-THPB, and THPB with two hydroxyl groups attaching to C3 and C10 showed one binding site to D1 receptors under the same conditions. However, the tested eleven THPB all manifested one binding site to D2 receptors in competition assay, and the 2-hydroxy-THPB had the most potent affinity for D2 receptors.

CONCLUSION

Dihydroxy-THPB with two hydroxyl groups attaching to C2 and C9 or C2 and C10 possess the intrinsic activity of agonist to D1 receptors, while the other THPB do not. The tested eleven THPB all are the antagonists of D2 receptors.

Authors+Show Affiliations

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

10072938

Citation

Guo, X, et al. "Characteristics of Tetrahydroprotoberberines On Dopamine D1 and D2 Receptors in Calf Striatum." Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica, vol. 18, no. 3, 1997, pp. 225-30.
Guo X, Wang LM, Liu J, et al. Characteristics of tetrahydroprotoberberines on dopamine D1 and D2 receptors in calf striatum. Zhongguo Yao Li Xue Bao. 1997;18(3):225-30.
Guo, X., Wang, L. M., Liu, J., & Jin, G. Z. (1997). Characteristics of tetrahydroprotoberberines on dopamine D1 and D2 receptors in calf striatum. Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica, 18(3), 225-30.
Guo X, et al. Characteristics of Tetrahydroprotoberberines On Dopamine D1 and D2 Receptors in Calf Striatum. Zhongguo Yao Li Xue Bao. 1997;18(3):225-30. PubMed PMID: 10072938.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Characteristics of tetrahydroprotoberberines on dopamine D1 and D2 receptors in calf striatum. AU - Guo,X, AU - Wang,L M, AU - Liu,J, AU - Jin,G Z, PY - 1997/5/1/pubmed PY - 1999/3/12/medline PY - 1997/5/1/entrez SP - 225 EP - 30 JF - Zhongguo yao li xue bao = Acta pharmacologica Sinica JO - Zhongguo Yao Li Xue Bao VL - 18 IS - 3 N2 - AIM: To study the characteristics of tetrahydroprotoberberines (THPB) on dopamine D1 and D2 receptors and elucidate their structure-activity relationship. METHODS: Radioligand assay in vitro with a two-site model program analysis. RESULTS: Four THPB with two hydorxyl groups on C2 and C9 or C2 and C10 exhibited RH and RL two binding sites to D1 receptors and guanosine triphosphate regulated the RH binding site of SPD and THPB-132A in competition assay, while eleven THPB including nonhydroxy-THPB, monohydroxy-THPB, and THPB with two hydroxyl groups attaching to C3 and C10 showed one binding site to D1 receptors under the same conditions. However, the tested eleven THPB all manifested one binding site to D2 receptors in competition assay, and the 2-hydroxy-THPB had the most potent affinity for D2 receptors. CONCLUSION: Dihydroxy-THPB with two hydroxyl groups attaching to C2 and C9 or C2 and C10 possess the intrinsic activity of agonist to D1 receptors, while the other THPB do not. The tested eleven THPB all are the antagonists of D2 receptors. SN - 0253-9756 UR - https://www.unboundmedicine.com/medline/citation/10072938/Characteristics_of_tetrahydroprotoberberines_on_dopamine_D1_and_D2_receptors_in_calf_striatum_ DB - PRIME DP - Unbound Medicine ER -