(R)-5-HYDROXY-2-(DIPROPYLAMINO)TETRALIN AND (S)-5-HYDROXY-2-(DIPROPYLAMINO)TETRALIN (5-OH DPAT) - ASSESSMENT OF OPTICAL PURITIES AND DOPAMINERGIC ACTIVITIES

被引：27

作者：

KARLSSON, A

BJORK, L

PETTERSSON, C

ANDEN, NE

HACKSELL, U

机构：

[1] UNIV UPPSALA,CTR BIOMED,DEPT ANALYT PHARMACEUT,BOX 574,S-75123 UPPSALA,SWEDEN

[2] UNIV UPPSALA,CTR BIOMED,DEPT ORGAN PHARMACEUT CHEM,S-75123 UPPSALA,SWEDEN

[3] UNIV UPPSALA,UPPSALA BIOMED CTR,DEPT MED PHARMACOL,S-75124 UPPSALA,SWEDEN

[4] KAROLINSKA INST,DEPT PHARMACOL,S-10401 STOCKHOLM 60,SWEDEN

来源：

CHIRALITY | 1990年 / 2卷 / 02期

关键词：

5‐OH DPAT; chiral ion pair chromatography; dopamine D[!sub]2[!/sub]‐receptor antagonist; N‐benzyloxycarbonylglycyl‐L‐proline (L‐ZGP); stereoselectivity;

D O I：

10.1002/chir.530020206

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Racemic 5‐hydroxy‐2‐(dipropylamino)tetralin (5‐OH DPAT), a potent and selective dopamine (DA) D2‐receptor agonist, was resolved into the enantiomers by a new method. The enantiomers of 5‐OH DPAT were determined by chiral ion‐pair chromatography using N‐benzyloxycarbonylglycyl‐L‐proline as the counter ion. The enantiomeric purity of (R)‐5‐OH DPAT was found to be > 99.7%. The ability of the enantiomers to change the rat brain DOPA levels was evaluated in vivo. The results indicate that (R)‐5‐OH DPAT is a weakly potent DA D2‐receptor antagonist. Copyright © 1990 Wiley‐Liss, Inc.

引用

收藏

页码：90 / 95

页数：6

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