Antagonists of the P2X7 Receptor. From Lead Identification to Drug Development

被引：126

作者：

Guile, Simon D. ^{[1
]}

Alcaraz, Lilian ^{[1
]}

Birkinshaw, Timothy N. ^{[1
]}

Bowers, Keith C. ^{[2
]}

Ebden, Mark R. ^{[1
]}

Furber, Mark ^{[1
]}

Stocks, Michael J. ^{[1
]}

机构：

[1] AstraZeneca R&D Charnwood, Dept Med Chem, Loughborough LE11 5RH, Leics, England

[2] AstraZeneca R&D Charnwood, Dept Biosci, Loughborough LE11 5RH, Leics, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 10期

关键词：

IN-VITRO ACTIVITY; POTENT ANTAGONIST; INTERLEUKIN-1-BETA RELEASE; BIOLOGICAL-ACTIVITY; NEUROPATHIC PAIN; ATP RECEPTOR; P2; RECEPTORS; DISCOVERY; PURINOCEPTOR; MATURATION;

D O I：

10.1021/jm801528x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

[No abstract available]

引用

页码：3123 / 3141

页数：19

共 116 条

[91] ATP acts as an agonist to promote stimulus-induced secretion of IL-1β and IL-18 in human blood [J].

Perregaux, DG ;

McNiff, P ;

Laliberte, R ;

Conklyn, M ;

Gabel, CA .

JOURNAL OF IMMUNOLOGY, 2000, 165 (08) :4615-4623

[92]

PFIZER PROD INC, 2004, Patent No. 2004058270

[93]

PFIZER PRODUCTS INC, 2004, Patent No. 2004099146

[94] Stimulation of P2 receptors causes release of IL-1β-loaded microvesicles from human dendritic cells [J].

Pizzirani, Cinzia ;

Ferrari, Davide ;

Chiozzi, Paola ;

Adinolfi, Elena ;

Sandona, Dorianna ;

Savaglio, Erika ;

Di Virgilio, Francesco .

BLOOD, 2007, 109 (09) :3856-3864

[95]

Ralevic V, 1998, PHARMACOL REV, V50, P413

[96] The permeabilizing ATP receptor, P2X(7) - Cloning and expression of a human cDNA [J].

Rassendren, F ;

Buell, GN ;

Virginio, C ;

Collo, G ;

North, RA ;

Surprenant, A .

JOURNAL OF BIOLOGICAL CHEMISTRY, 1997, 272 (09) :5482-5486

[97] Potent P2X7 receptor antagonists:: Tyrosyl derivatives synthesized using a sequential parallel synthetic approach [J].

Ravi, RG ;

Kertesy, SB ;

Dubyak, GR ;

Jacobson, KA .

DRUG DEVELOPMENT RESEARCH, 2001, 54 (02) :75-87

[98]

RENOVIS INC, 2007, Patent No. 2007109182

[99] Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor [J].

Romagnoli, R ;

Baraldi, PG ;

Pavani, MG ;

Tabrizi, MA ;

Moorman, AR ;

Di Virgilio, F ;

Cattabriga, E ;

Pancaldi, C ;

Gessi, S ;

Borea, PA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (22) :5709-5712

[100]

Romagnoli R, 2008, EXPERT OPIN THER TAR, V12, P647, DOI [10.1517/14728222.12.5.647, 10.1517/14728222.12.5.647 ]

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