1-BENZAZEPINE DERIVATIVES ACTING AS ATP-DEPENDENT POTASSIUM CHANNELS ANTAGONISTS

被引：32

作者：

CORBEL, JC ^{[1
]}

URIAC, P ^{[1
]}

HUET, J ^{[1
]}

MARTIN, CAE ^{[1
]}

ADVENIER, C ^{[1
]}

机构：

[1] UNIV PARIS 05,INST BIOMED CORDELIERS,PHARMACOL LAB,F-75270 PARIS 06,FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 30卷 / 01期

关键词：

1-BENZAZEPINE; ATP-DEPENDENT K+-CHANNEL ANTAGONIST;

D O I：

10.1016/0223-5234(96)88204-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In order to select between various pharmacological activities related to the 1-benzazepine nucleus, a set of 1-benzazepine derivatives bearing different N-1 or C-2 substituents were synthesized and tested in vitro as ATP-dependent Kf-channel antagonists on isolated guinea-pig trachea. Cumulative concentration curves to cromakalim were constructed in the absence or presence of the various compounds tested in comparison with glibenclamide. Products bearing N-1 substituents, especially (2-imidazolinyl)methyl showed a non-competitive antagonism towards ATP-dependent K+ channels.

引用

页码：3 / 13

页数：11

共 30 条

[1]

BARRETT WE, 1969, ARCH INT PHARMACOD T, V182, P65

[2]

BARSKY LI, 1971, J MED CHEM, V14, P40

[3]

BEKE D, 1962, BER DTSCH CHEM GES, V95, P2122

[4] POTASSIUM CHANNELS AND AIRWAY FUNCTION - NEW THERAPEUTIC PROSPECTS [J].

BLACK, JL ;

BARNES, PJ .

THORAX, 1990, 45 (03) :213-218

[5]

BONNIC J, 1974, CR ACAD SCI C CHIM, V278, P1461

[6]

BROWN HC, 1966, J AM CHEM SOC, V87, P1464

[7]

COLATSKY TJ, 1992, POTASSIUM CHANNEL MO, P304

[8]

CORBEL JC, 1984, 20ES REC INT CHIM TH

[9]

DUNNE MJ, 1992, POTASSIUM CHANNEL MO, P110

[10] UBER EINE NEUARTIGE ISOMERISIERUNG DES DELTA-2-CYCLOPENTENYL-ACETONOXIMS - (DARSTELLUNG UND EIGENSCHAFTEN BICYCLISCHER PYRROLIN-DERIVATE) .3. [J].

GRIOT, R ;

WAGNERJAUREGG, T .

HELVETICA CHIMICA ACTA, 1959, 42 (03) :605-628

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