A STUDY OF CRYSTAL STRUCTURE OF TETRAHYDROPROTOBERBERINES AND EFFECTS ON DEPAMINE RECEPTOR D-1 AND D-2 SUBTYPES IN BRAIN

摘要

＜正＞ The molecular structure of tetrahydroberberine（THB）is determined by X-ray diffraction method.By the analysis of the crystal structure of four l-tetrahydroprotoberberines（l-THPB）,i.e.l-tetrahydropalmatine（l-THP）,l-corydalamine（l-CDL）,l-stepholidine（l-SPD）,l-THB and the QSARcalculation of Hansch approach,we find that the negative correlation exists between A-D ring dihedralangles of THPB crystal structures and the potency of the inhibition of D-1 and D-2 receptors.The re-sults suggest that the smaller the A-D dihedral angle,the easier the binding to the DA receptors.The cal-culation results also show that the activity of the l-THPB toward D-1 receptor is higher by 4.5—6.1times than that toward D-2 receptor.