Concepedia

Discovery of Potent and Selective Adamantane-Based Small-Molecule P2X<sub>7</sub>Receptor Antagonists/Interleukin-1β Inhibitors

Mark Furber, Lilian Alcaraz, Janice Bent, Armin Beyerbach, Keith Bowers, Martin Braddock, Moya Caffrey, David E. Cladingboel, John Collington, David K. Donald,

Journal of Medicinal Chemistry · 2007 · 59 citations · 11 references

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Concepts

Abstract

A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.

References

11

Rapid Secretion of Interleukin-1β by Microvesicle Shedding

Amanda B. Mackenzie, Heather L. Wilson, Endre Kiss‐Toth et al. · Immunity · 2001 · 852 citations · Full text

, , +11

Interleukin-1 beta maturation and release in response to ATP and nigericin. Evidence that potassium depletion mediated by these agents is a necessary and common feature of their activity.

David G. Perregaux, Christopher A. Gabel · Journal of Biological Chemistry · 1994 · 759 citations · Full text

, , +17

Tissue distribution of the P2X7 receptor

Ginetta Collo, S. Neidhart, Eric Kawashima et al. · Neuropharmacology · 1997 · 498 citations

, , +13

Absence of the P2X7 Receptor Alters Leukocyte Function and Attenuates an Inflammatory Response

Jeffrey M. Labasi, Nina Petrushova, Carol Donovan et al. · The Journal of Immunology · 2002 · 487 citations · Full text

, , +17

The isoquinoline derivative KN‐62 a potent antagonist of the P2Z‐receptor of human lymphocytes

Caroline E. Gargett, James S. Wiley · British Journal of Pharmacology · 1997 · 191 citations · Full text

, , +17