Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity

被引：30

作者：

Venkatesan, Aranapakam M. ^{[1
]}

Dos Santos, O. ^{[1
]}

Ellingboe, John ^{[1
]}

Evrard, Deborah A. ^{[2
]}

Harrison, Boyd L. ^{[2
]}

Smith, Deborah L. ^{[3
]}

Scerni, Rosemary ^{[3
]}

Hornby, Geoffrey A. ^{[3
]}

Schechter, Lee E. ^{[3
]}

Andree, Terrence H. ^{[3
]}

机构：

[1] Wyeth Res, Chem Sci, Pearl River, NY 10965 USA

[2] Wyeth Res, Chem Sci, Princeton, NJ 08543 USA

[3] Wyeth Res, Neurosci Discovery Res, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

SSRI; 5HT-1A; Benzofuran; NEXT-GENERATION; ANTIDEPRESSANT DRUGS; REUPTAKE INHIBITORS; MAJOR DEPRESSION; FRONTAL-CORTEX; CITALOPRAM; DISCOVERY; PINDOLOL; ANTAGONISTS; BINDING;

D O I：

10.1016/j.bmcl.2009.12.093

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several benzofuran derivatives linked to a 3-indoletetrahydropyridine through an alkyl chain were prepared and evaluated for serotonin transporter and 5-HT1A receptor affinities. Their design, synthesis and structure-activity relationships are described. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：824 / 827

页数：4

共 17 条

[1]

ARBORELIUS L, 1995, N-S ARCH PHARMACOL, V352, P157

[2] Acceleration of the effect of selected antidepressant drugs in major depression by 5-HT1A antagonists [J].

Artigas, F ;

Romero, L ;

deMontigny, C ;

Blier, P .

TRENDS IN NEUROSCIENCES, 1996, 19 (09) :378-383

[3]

ARTIGAS F, 1994, ARCH GEN PSYCHIAT, V51, P248

[4]

Blier P, 1998, J CLIN PSYCHIAT, V59, P16

[5] EFFECTIVENESS OF PINDOLOL WITH SELECTED ANTIDEPRESSANT DRUGS IN THE TREATMENT OF MAJOR DEPRESSION [J].

BLIER, P ;

BERGERON, R .

JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY, 1995, 15 (03) :217-222

[6]

CHAN AWY, 2002, Patent No. 2002092602

[7] [H-3] PAROXETINE BINDING IN RAT FRONTAL-CORTEX STRONGLY CORRELATES WITH [H-3] 5-HT UPTAKE - EFFECT OF ADMINISTRATION OF VARIOUS ANTIDEPRESSANT TREATMENTS [J].

CHEETHAM, SC ;

VIGGERS, JA ;

SLATER, NA ;

HEAL, DJ ;

BUCKETT, WR .

NEUROPHARMACOLOGY, 1993, 32 (08) :737-743

[8] Effect of chronic fluoxetine and WAY-100635 treatment on serotonergic neurotransmission in the frontal cortex [J].

Dawson, LA ;

Nguyen, HQ ;

Smith, DL ;

Schechter, LE .

JOURNAL OF PSYCHOPHARMACOLOGY, 2002, 16 (02) :145-152

[9] Characterization of 5-HT1A receptor functional coupling in cells expressing the human 5-HT1A receptor as assessed with the cytosensor microphysiometer [J].

Dunlop, J ;

Zhang, YX ;

Smith, DL ;

Schechter, LE .

JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, 1998, 40 (01) :47-55

[10]

HJOORTH S, 1996, BEHAV BRAIN RES, V73, P281

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