Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles:: new selective ligands of the 5-HT7 receptor

被引：38

作者：

Kikuchi, C ^{[1
]}

Hiranuma, T ^{[1
]}

Koyama, M ^{[1
]}

机构：

[1] Meiji Seika Kaisha Ltd, Pharmaceut Res Ctr, Kohoku Ku, Yokohama, Kanagawa 2228567, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(02)00485-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and the affinity for the 5-HT7 receptor and other receptors of a novel series of fused-ring tetrahydropyridine derivatives are described. Some of the compounds showed high affinity for the 5-HT7 receptor. Tetrahydrothienopyridylbutyl-tetrahydrobenzindoles 5d and 5h are potent ligands for the 5-HT7 receptor, with high selectivity over the 5-HT2 receptor and other receptors. These compounds should be useful tools for clarifying the biological role of the 5-HT7 receptor. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2549 / 2552

页数：4

共 31 条

[1]

BARD JA, 1993, J BIOL CHEM, V268, P23422

[2]

Branchek T. A., 1994, British Journal of Pharmacology, V112, p100P

[3]

Cushing DJ, 1996, J PHARMACOL EXP THER, V277, P1560

[4]

Frankel S, 1920, BIOCHEM Z, V110, P234

[5] COMPARATIVE STUDY OF AROMATIC CHARACTER OF FURAN, THIOPHENE, SELENOPHEN, AND TELLUROPHEN [J].

FRINGUEL.F ;

MARINO, G ;

TATICCHI, A ;

GRANDOLI.G .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 2, 1974, (04) :332-337

[6] DEVELOPMENT OF A RADIOLIGAND BINDING ASSAY FOR 5-HT(4)-RECEPTORS IN GUINEA-PIG AND RAT-BRAIN [J].

GROSSMAN, CJ ;

KILPATRICK, GJ ;

BUNCE, KT .

BRITISH JOURNAL OF PHARMACOLOGY, 1993, 109 (03) :618-624

[7] A receptor autoradiographic and in situ hybridization analysis of the distribution of the 5-ht(7) receptor in rat brain [J].

Gustafson, EL ;

Durkin, MM ;

Bard, JA ;

Zgombick, J ;

Branchek, TA .

BRITISH JOURNAL OF PHARMACOLOGY, 1996, 117 (04) :657-666

[8] MOLECULAR PHARMACOLOGY OF 5-HT1 AND 5-HT2 RECOGNITION SITES IN RAT AND PIG BRAIN MEMBRANES - RADIOLIGAND BINDING-STUDIES WITH [H-3] 5-HT, [H-3] 8-OH-DPAT, (-) [I-125] IODOCYANOPINDOLOL, [H-3] MESULERGINE AND [H-3] KETANSERIN [J].

HOYER, D ;

ENGEL, G ;

KALKMAN, HO .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1985, 118 (1-2) :13-23

[9] Tetrahydrobenzindoles:: Selective antagonists of the 5-HT7 receptor [J].

Kikuchi, C ;

Nagaso, H ;

Hiranuma, T ;

Koyama, M .

JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (04) :533-535

[10] 2a-[4-(tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives:: New selective antagonists of the 5-hydroxytryptamine7 receptor [J].

Kikuchi, C ;

Ando, T ;

Watanabe, T ;

Nagaso, H ;

Okuno, M ;

Hiranuma, T ;

Koyama, M .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (11) :2197-2206

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