SYNTHESIS AND PHARMACOLOGICAL CHARACTERIZATION OF ABT-200 - A PUTATIVE NOVEL ANTIDEPRESSANT COMBINING POTENT ALPHA-2 ANTAGONISM WITH MODERATE NE UPTAKE INHIBITION

被引:16
作者
ZELLE, RE [1 ]
HANCOCK, AA [1 ]
BUCKNER, SA [1 ]
BASHA, FZ [1 ]
TIETJE, K [1 ]
DEBERNARDIS, JF [1 ]
MEYER, MD [1 ]
机构
[1] ABBOTT LABS,PHARMACEUT DISCOVERY D47C,ABBOTT PK,IL 60064
关键词
D O I
10.1016/S0960-894X(01)80353-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
ABT-200, (+/-)-(1'R*, 3R*)-3-phenyl-1-[(1',2',3',4'-tetrahydro-5',6'-methylenedioxy-1'-naphthalenyl)methyl]pyrrolidine, (1a/b) represents the first example of a new structural class of potent alpha-2 antagonists which possess the additional property of norepinephrine (NE) uptake inhibition. This profile of combined activities is expected to have utility in the treatment of depression.
引用
收藏
页码:1319 / 1322
页数:4
相关论文
共 13 条
[1]  
CASS WA, IN PRESS SYNAPSE
[2]  
CONSTANTINE JW, 1982, EUR J PHARMACOL, V85, P325, DOI 10.1016/0014-2999(82)90219-9
[3]   CONFORMATIONALLY DEFINED ADRENERGIC AGENTS .5. RESOLUTION, ABSOLUTE-CONFIGURATION, AND PHARMACOLOGICAL CHARACTERIZATION OF THE ENANTIOMERS OF 2-(5,6-DIHYDROXY-1,2,3,4-TETRAHYDRO-1-NAPHTHYL)IMIDAZOLINE - A POTENT AGONIST AT ALPHA-ADRENOCEPTORS [J].
DEBERNARDIS, JF ;
KERKMAN, DJ ;
ARENDSEN, DL ;
BUCKNER, SA ;
KYNCL, JJ ;
HANCOCK, AA .
JOURNAL OF MEDICINAL CHEMISTRY, 1987, 30 (06) :1011-1017
[4]  
DENNIS T, 1987, J PHARMACOL EXP THER, V241, P642
[5]   SELECTIVITY OF BLOCKING-AGENTS FOR PRESYNAPTIC AND POSTSYNAPTIC ALPHA-ADRENOCEPTORS [J].
DOXEY, JC ;
SMITH, CFC ;
WALKER, JM .
BRITISH JOURNAL OF PHARMACOLOGY, 1977, 60 (01) :91-96
[6]   IDAZOXAN (RX-781094) SELECTIVELY ANTAGONIZES ALPHA-2-ADRENOCEPTORS ON RAT CENTRAL NEURONS [J].
FREEDMAN, JE ;
AGHAJANIAN, GK .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1984, 105 (3-4) :265-272
[7]  
HANCOCK AA, UNPUB J PHARM EXP TH
[8]  
LHEUREUX R, 1986, J NEUROCHEM, V46, P1794
[9]  
Meltzer HY, 1987, PSYCHOPHARMACOLOGY 3
[10]   EVALUATION OF STUDIES ON PLATELET ALPHA-2 ADRENOCEPTORS IN DEPRESSIVE-ILLNESS [J].
PILETZ, JE ;
SCHUBERT, DSP ;
HALARIS, A .
LIFE SCIENCES, 1986, 39 (18) :1589-1616