SUBSTITUTED 3-PHENYLPIPERIDINES - NEW CENTRALLY ACTING DOPAMINE AUTORECEPTOR ANTAGONISTS

被引：46

作者：

SONESSON, C

WATERS, N

SVENSSON, K

CARLSSON, A

SMITH, MW

PIERCEY, MF

MEIER, E

WIKSTROM, H

机构：

[1] UPJOHN CO,UPJOHN LABS,KALAMAZOO,MI 49001

[2] H LUNDBECK & CO AS,DK-2500 COPENHAGEN,DENMARK

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 21期

关键词：

D O I：

10.1021/jm00073a021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The (+)-and (-)-enantiomer of compounds 4 and 5 were synthesized and tested for central dopamine (DA) receptor stimulating activity, using biochemical and behavioral tests in rats. Based on the available data the (-)-enantiomers of 4 and 5 are characterized as centrally acting DA autoreceptor antagonists with oral activity. They display a similar pharmacological profile as the prototype DA autoreceptor antagonists (+)-1 and (+)-2 and show a certain preference for the D3 DA receptor antagonist binding site.

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页码：3188 / 3196

页数：9

相关论文

共 52 条

[1]

AGHAJANIAN GK, 1972, P S DRUG ABUSE METAB, P115

[2] ADRENERGIC MECHANISMS [J].

ANDEN, NE ;

CARLSSON, A ;

HAGGENDAL, J .

ANNUAL REVIEW OF PHARMACOLOGY, 1969, 9 :119-+

[3] SIMULTANEOUS MEASUREMENT OF TYROSINE AND TRYPTOPHAN HYDROXYLASE-ACTIVITIES IN BRAIN IN-VIVO USING AN INHIBITOR OF AROMATIC AMINO-ACID DECARBOXYLASE [J].

CARLSSON, A ;

ATACK, CV ;

LINDQVIST, M ;

KEHR, W ;

DAVIS, JN .

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1972, 275 (02) :153-+

[4]

CARLSSON A, 1978, PSYCHOPHARMACOLOGY G, P1057

[5] NICKEL CATALYZED CONVERSION OF PHENOL TRIFLATES INTO AROMATIC NITRILES AND ACIDS [J].

CHAMBERS, MRI ;

WIDDOWSON, DA .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1989, (07) :1365-1366

[6]

CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099

[7] A 2ND MOLECULAR-FORM OF D2 DOPAMINE RECEPTOR IN RAT AND BOVINE CAUDATE-NUCLEUS [J].

CHIO, CL ;

HESS, GF ;

GRAHAM, RS ;

HUFF, RM .

NATURE, 1990, 343 (6255) :266-269

[8] PALLADIUM-CATALYZED COUPLING OF ARYL TRIFLATES WITH ORGANOSTANNANES [J].

ECHAVARREN, AM ;

STILLE, JK .

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1987, 109 (18) :5478-5486

[9] NOVEL PIPERIDINE SIGMA RECEPTOR LIGANDS AS POTENTIAL ANTIPSYCHOTIC-DRUGS [J].

GILLIGAN, PJ ;

CAIN, GA ;

CHRISTOS, TE ;

COOK, L ;

DRUMMOND, S ;

JOHNSON, AL ;

KERGAYE, AA ;

MCELROY, JF ;

ROHRBACH, KW ;

SCHMIDT, WK ;

TAM, SW .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (23) :4344-4361

[10] N-ALKYLATED 2-AMINOTETRALINS - CENTRAL DOPAMINE-RECEPTOR STIMULATING ACTIVITY [J].

HACKSELL, U ;

SVENSSON, U ;

NILSSON, JLG ;

HJORTH, S ;

CARLSSON, A ;

WIKSTROM, H ;

LINDBERG, P ;

SANCHEZ, D .

JOURNAL OF MEDICINAL CHEMISTRY, 1979, 22 (12) :1469-1475

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