Structure-activity relationship studies of CNS agents .32. Effect of structural modifications in 1-arylpiperazine derivatives on alpha(1)-adrenoreceptor affinity

被引:15
作者
Mokrosz, MJ
Paluchowska, MH
CharakchievaMinol, S
Bien, A
机构
[1] Institute of Pharmacology, Polish Academy of Sciences, 31-343 Kraków
关键词
1-arylpiperazines; alpha(1)-adrenergic receptor affinity; 5-HT1A/alpha(1) receptor selectivity; structural modifications;
D O I
10.1002/ardp.19973300605
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The alpha(1)-adrenergic and 5-HT1A serotonergic receptor affinities of a series of 1-arylpiperazines are presented. The role of the spacer and the influence of the terminal substituents on the alpha(1)-adrenoreceptor affinity and the 5-HT1A/alpha 1 receptor selectivity are discussed.
引用
收藏
页码:177 / 180
页数:4
相关论文
共 28 条
[11]   STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CENTRAL-NERVOUS-SYSTEM AGENTS .13. 4-[3-(BENZOTRIAZOL-1-YL)PROPYL]-1-(2-METHOXYPHENYL)PIPERAZINE, A NEW PUTATIVE 5-HT1A RECEPTOR ANTAGONIST, AND ITS ANALOGS [J].
MOKROSZ, JL ;
PALUCHOWSKA, MH ;
CHOJNACKAWOJCIK, E ;
FILIP, M ;
CHARAKCHIEVAMINOL, S ;
DERENWESOLEK, A ;
MOKROSZ, MJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (17) :2754-2760
[12]   Structure-activity relationship studies of CNS agents .29. N-methylpiperazino-substituted derivatives of quinazoline, phthalazine and quinoline as novel alpha(1), 5-HT1A and 5-HT2A receptor ligands [J].
Mokrosz, JL ;
Duszynska, B ;
CharakchievaMinol, S ;
Bojarski, AJ ;
Mokrosz, MJ ;
Wydra, RL ;
Janda, L ;
Strekowski, L .
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1996, 31 (12) :973-980
[13]   STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CNS AGENTS .19. QUANTITATIVE-ANALYSIS OF THE ALKYL CHAIN EFFECTS ON THE 5-HT1A AND 5-HT2 RECEPTOR AFFINITIES OF 4-ALKYL-1-ARYLPIPERAZINES AND THEIR ANALOGS [J].
MOKROSZ, JL ;
MOKROSZ, MJ ;
CHARAKCHIEVAMINOL, S ;
PALUCHOWSKA, MH ;
BOJARSKI, AJ ;
DUSZYNSKA, B .
ARCHIV DER PHARMAZIE, 1995, 328 (02) :143-148
[14]   Struture-activity relationship studies of CNS agents .26. 4-[2-(Cycloalkanecarboxamido)ethyl]-1-(2-methoxyphenyl)-piperazines: High-affinity 5-HT1A agonists [J].
Mokrosz, JL ;
Paluchowska, MH ;
Klodzinska, A ;
CharakchievaMinol, S ;
ChojnackaWojcik, E .
ARCHIV DER PHARMAZIE, 1995, 328 (11-12) :770-774
[15]  
MOKROSZ JL, 1994, PHARMAZIE, V49, P801
[16]  
MOKROSZ MJ, IN PRESS BIIORG MED
[17]  
Mokrosz MJ, 1994, MED CHEM RES, V4, P161
[18]   4,6-Di(heteroaryl)-2-(N-methylpiperazino)pyrimidines as new, potent 5-HT2A receptor ligands: A verification of the topographic model [J].
Mokroz, MJ ;
Strekowski, L ;
Kozak, WX ;
Duszynska, B ;
Bojarski, AJ ;
Klodzinska, A ;
Czarny, A ;
Cegla, MT ;
DerenWesolek, A ;
ChojnackaWojcik, E ;
Dove, S ;
Mokrosz, JL .
ARCHIV DER PHARMAZIE, 1995, 328 (09) :659-666
[19]  
MOKSA J, 1996, PHARMAZIE, V51, P72
[20]   Structure-activity relationship studies of CNS agents .31. Analogs of MP 3022 with a different number of nitrogen atoms in the heteroaromatic fragment - New 5-HT1A receptor ligands [J].
Paluchowska, MH ;
DerenWesolek, A ;
Mokrosz, JL ;
CharakchievaMinol, S ;
ChojnackaWojcik, E .
ARCHIV DER PHARMAZIE, 1996, 329 (10) :451-456