N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers

被引：19

作者：

Hu, LY

Ryder, TR

Rafferty, MF

Cody, WL

Lotarski, SM

Miljanich, GP

Millerman, E

Rock, DM

Song, YT

Stoehr, SJ

Taylor, CP

Weber, ML

Szoke, BG

Vartanian, MG

机构：

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

[2] Elan Pharmaceut Inc, Menlo Park, CA 94025 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(99)00100-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke amid pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：907 / 912

页数：6

共 15 条

[1]

Bowersox SS, 1997, BRAIN RES, V747, P343

[2]

Bowersox SS, 1996, J PHARMACOL EXP THER, V279, P1243

[3]

BOWERSOX SS, 1994, DRUG NEWS PERSPECT, V7, P261

[4]

DESARRO GB, 1988, BRIT J PHARMACOL, V93, P247

[5]

GILMORE J, 1995, ANNU REP MED CHEM, V30, P51

[6] Behavioural and anticonvulsant effects of Ca2+ channel toxins in DBA/2 mice [J].

Jackson, HC ;

Scheideler, MA .

PSYCHOPHARMACOLOGY, 1996, 126 (01) :85-90

[7]

KWAPISZEWSKI W, 1994, ACTA POLINIAE PHARM, V51, P227

[8]

Meldrum B S, 1994, Neurology, V44, pS14

[9]

MILJANICH GP, 1995, ANN REV PHARM TOXICO, V35, P704

[10] CALCIUM-CHANNEL DIVERSITY AND NEUROTRANSMITTER RELEASE - THE OMEGA-CONOTOXINS AND OMEGA-AGATOXINS [J].

OLIVERA, BM ;

MILJANICH, GP ;

RAMACHANDRAN, J ;

ADAMS, ME .

ANNUAL REVIEW OF BIOCHEMISTRY, 1994, 63 :823-867

← 1 2 →