Identification and characterization of m4 selective muscarinic antagonists

被引：41

作者：

Augelli-Szafran, CE

Jaen, JC

Moreland, DW

Nelson, CB

Penvose-Yi, JR

Schwarz, RD

机构：

[1] Parke Davis Pharmaceut Res, Dept Med Chem, Ann Arbor, MI 48105 USA

[2] Parke Davis Pharmaceut Res, Dept Pharmacol, Ann Arbor, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(98)00351-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82-fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1991 / 1996

页数：6

共 15 条

[1]

Adamson D. W., 1954, U.S. Patent, Patent No. 2682543

[2] Muscarinic receptor subtype selective toxins [J].

Adem, A ;

Karlsson, E .

LIFE SCIENCES, 1997, 60 (13-14) :1069-1076

[3]

[Anonymous], 1958, Patent US, Patent No. 2852527

[4]

BEER JS, 1951, J CHEM SOC, P2029

[5]

BOLDEN C, 1992, J PHARMACOL EXP THER, V260, P576

[6]

BUCKLEY NJ, 1989, MOL PHARMACOL, V35, P469

[7]

Cohen M. P., 1972, U.S. Patent, Patent No. [3,649,626, 3649626]

[8]

DORJE F, 1991, J PHARMACOL EXP THER, V256, P727

[9]

GULLAND JM, 1929, J CHEM SOC, V36, P1791

[10]

MARCHELLI R, 1969, CAN J CHEM, V47, P4376

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