3-pyridylethanolamines:: Potent and selective human β3 adrenergic receptor agonists

被引：30

作者：

Naylor, EM ^{[1
]}

Colandrea, VJ

Candelore, MR

Cascieri, MA

Colwell, LF

Deng, LP

Feeney, WP

Forrest, MJ

Hom, GJ

MacIntyre, DE

Strader, CD

Tota, L

Wang, PR

Wyvratt, MJ

Fisher, MH

Weber, AE

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Biochem & Physiol, Rahway, NJ 07065 USA

[3] Merck Res Labs, Dept Pharmacol, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Lab Anim Resources, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(98)00571-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The 3-pyridylethanolamine L-757,793 is a potent beta(3) AR agonist (EC50 6.3 nM, 70% activation) with 1,300- and 500-fold selectivity over binding to the beta(1) and beta(2) ARs, respectively. L-757,793 stimulated lipolysis in rhesus monkeys (ED50 0.2 mg/kg) with a maximum response equivalent to that elicited by isoproterenol. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3087 / 3092

页数：6

共 15 条

[1]

Arch JRS, 1996, INT J OBESITY, V20, P191

[2] ATYPICAL BETA-ADRENOCEPTOR ON BROWN ADIPOCYTES AS TARGET FOR ANTI-OBESITY DRUGS [J].

ARCH, JRS ;

AINSWORTH, AT ;

CAWTHORNE, MA ;

PIERCY, V ;

SENNITT, MV ;

THODY, VE ;

WILSON, C ;

WILSON, S .

NATURE, 1984, 309 (5964) :163-165

[3]

CLAUS TH, 1995, ANNU REP MED CHEM, V30, P189

[4]

Dow R L, 1997, Expert Opin Investig Drugs, V6, P1811, DOI 10.1517/13543784.6.12.1811

[5] A selective human β3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys [J].

Fisher, MH ;

Amend, AM ;

Bach, TJ ;

Barker, JM ;

Brady, EJ ;

Candelore, MR ;

Carroll, D ;

Cascieri, MA ;

Chiu, SHL ;

Deng, LP ;

Forrest, MJ ;

Hegarty-Friscino, B ;

Guan, XM ;

Hom, GJ ;

Hutchins, JE ;

Kelly, LJ ;

Mathvink, RJ ;

Metzger, JM ;

Miller, RR ;

Ok, HO ;

Parmee, ER ;

Saperstein, R ;

Strader, CD ;

Stearns, RA ;

Thompson, GM ;

Tota, L ;

Vicario, PP ;

Weber, AE ;

Woods, JW ;

Wyvratt, MJ ;

Zafian, PT ;

MacIntyre, DE .

JOURNAL OF CLINICAL INVESTIGATION, 1998, 101 (11) :2387-2393

[6]

FISHER MH, 1996, Patent No. 5541197

[7] CLONING OF THE CDNA FOR THE HUMAN BETA-1-ADRENERGIC RECEPTOR [J].

FRIELLE, T ;

COLLINS, S ;

DANIEL, KW ;

CARON, MG ;

LEFKOWITZ, RJ ;

KOBILKA, BK .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (22) :7920-7924

[8] CDNA FOR THE HUMAN BETA-2-ADRENERGIC RECEPTOR - A PROTEIN WITH MULTIPLE MEMBRANE-SPANNING DOMAINS AND ENCODED BY A GENE WHOSE CHROMOSOMAL LOCATION IS SHARED WITH THAT OF THE RECEPTOR FOR PLATELET-DERIVED GROWTH-FACTOR [J].

KOBILKA, BK ;

DIXON, RAF ;

FRIELLE, T ;

DOHLMAN, HG ;

BOLANOWSKI, MA ;

SIGAL, IS ;

YANGFENG, TL ;

FRANCKE, U ;

CARON, MG ;

LEFKOWITZ, RJ .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (01) :46-50

[9]

LIGGETT SB, 1992, MOL PHARMACOL, V42, P634

[10]

Lowell BB, 1997, ANNU REV MED, V48, P307

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