Merck + Co., Inc.

Robert G Johnson

Christopher A Salvatore

Marlene A Jacobson

Christopher J Luneau

Stephen E DeLaszlo

Tsuneo Fujita

Christopher F Reilly

The invention concerns recombinant human adenosine receptors A1, A2a, A2b and A3 which have been prepared by cDNA cloning and polymerase chain reaction techniques. The invention also concerns expression systems for these receptors and an assay using the expression systems. The recombinant adenosine receptors comprising the invention can be utililized in an assay to identify and evaluate entities that bind to or enhance binding to adenosine receptors.

Human adenosine receptors

Human A3 adenosine receptors

The invention concerns the identification on eosinophils of the A3 adenosine receptor subtype and the blockade of said receptor in order to achieve inhibition of eosinophil activation and degranulation.

Inhibition of eosinophil activation through A3 adenosine receptor

The invention concerns recombinant human adenosine receptors A1, A2a, A2b and A3 which have been prepared by cDNA cloning and polymerase chain reaction techniques. The invention also concerns expression systems for these receptors and an assay using the expression systems. The recombinant adenosine receptors comprising the invention can be utilized in an assay to identify and evaluate entities that bind to or enhance binding to adenosine receptors.

Human A2B adenosine receptor assay

Novel disubstituted 6-aminoquinazolinones of the Formula ##STR1## are useful as angiotensin-II receptor (subtype 2) antagonists (AT.sub.2 antagonists) alone or in combination with heparin, and can act to suppress the vascular stenosis which commonly occurs during the development of atherosclerosis and the restenosis following arterial angioplasty, stent placement, bypass surgery, heart transplantation or endarterectomy.

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Rosemont, PA, United States of America

Robert G Johnson