Merck + Co., Inc.

Thomas M Connolly

Harold G Selnick

Daniel F Veber

Ruth F Nutt

James C Barrow

Philippe G Nantermet

Dong-Mei Feng

Robert J Gould

Paul M Keller

Lloyd H Waxman

Jerzy Karczewski

David A Claremon

John Howard Hutchinson

Nigel J Liverton

Roger M Freidinger

Michael J Breslin

John W Butcher

David G Melillo

Michael P Neeper

Kenneth S Koblan

Andrew M Stern

Dennis C Dean

Kristen L Glass

Matthew J Kostura

The present invention is directed to the radioligand compound, [S]-radiolabeled (+)-N-[1'-(6-cyano-1,2,3,4-tetrahydro-2(R)-naphthalenyl)-3,4-dihydro-4(R)-hydoxyspiro[2H-1-benzopyran-2,4&#x2032;-piperidin]-6-yl]methanesulfonamide. Also within the scope of this invention is a method for identifying compounds that bind to the Ichannel, and may have antiarrhythmic activity.

Radioligand and binding assay

Thrombin receptor antagonists

Thrombin receptor binding peptides

The radioligands are six amino acid peptides having iodinated tyrosine at amino acid position six, including Ala-pFPhe-hArg-Cha-hArg-Tyr(I)-NH.sub.2, which mimic the activated form of the thrombin receptor protein. Thrombin receptor radioligands of the present invention are useful for screening for thrombin receptor antagonists.

Thrombin receptor radioligands

A protein which inhibits collagen-stimulated platelet aggregation. The protein has a molecular weight of approximately 17,000. A method of isolating the protein from Ornithodoros moubata and using the protein to prevent or delay blood coagulation by blocking the stimulation of platelet aggregation by collagen is also described. The protein is useful in the prevention, prophylaxis, therapy and treatment of thrombotic diseases.

Protein for inhibiting collagen-stimulated platelet aggregation

A protein isolated from crude Haementeria officinalis extract which blocks stimulation of platelet aggregation by collagen. The protein has a molecular weight of approximately 16,000. A method of isolating the protein and using the protein to prevent or delay blood coagulation by blocking the stimulation of platelet aggregation by collagen is also described. The protein is useful in the prevention, prophylaxis, therapy and treatment of thrombotic diseases.

The invention comprises proteinaceous substances isolated from crude Ornithodoros moubata extract which inhibit adhesion of platelets to collagen. These substances do not inhibit platelet adhesion to fibrinogen, and are therefore particularly useful for inhibiting adhesion of platelets to collagen when simultaneous inhibition of platelet adhesion to fibrinogen is undesired. They are particularly useful in the prevention, prophylaxis, therapy and treatment of thrombotic diseases.

Proteins for inhibiting adhesion of platelets to collagen

A method for blocking platelet adhesion to collagen by contacting platelets with a polypeptide having one of the following sequences:

Method for blocking platelet adhesion to collagen

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Harleysville, PA, United States of America

Thomas M Connolly