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Specific Binding of the New Stable Epoprostenol Analogue Beraprost Sodium to Prostacyclin Receptors on Human and Rat Platelets

Specific Binding of the New Stable Epoprostenol Analogue Beraprost Sodium to Prostacyclin Receptors on Human and Rat Platelets

N Kajikawa, K Nogimori, T Murata, S Nishio, S Uchiyama

Arzneimittelforschung. 1989 Apr;39(4):495-9.

PMID: 2665758

Abstract:

Binding of beraprost sodium (sodium dl-4-[(1R,2R,3aS,8bS)-1,2,3a,8b-tetrahydro-2-hydroxy-1-[(3S, 4RS)- 3-hydroxy-4-methyl-oct-6-yne-(E)-1-enyl] -5- cyclopenta[b]benzofuranyl]butyrate, TRK-100), a new potent antithrombotic agent, to washed platelets of humans and rats was studied. [11-3H]-TRK-100 binding was rapid, reversible, saturable, and highly specific. Scatchard analysis of concentration-dependent binding to human platelets revealed a single class of specific binding sites with an equilibrium dissociation constant (Kd) of 133 nmol/l and a maximal concentration of binding sites (Bmax) of 46 fmol/10(8) platelets (275 sites/cell). Similar binding was observed on rat platelets. The Kd and Bmax were 66 nmol/l and 124 fmol/10(8) platelets (750 sites/cell), respectively. Competitive studies indicated that TRK-100 was 1.5 times less active than prostacyclin (epoprostenol, PGI2), but was 3 times more potent than PGE1 in displacing [3H]-TRK-100 from the binding sites on rat platelets. PGE2, PGD2, PGF2 alpha, and pinane thromboxane A2, a stable thromboxane A2 analogoue, had no affinity for the binding sites. The relative affinity of the four enantiomers of TRK-100--APS-314d, 315d, 3141 and 3151--for the binding sites was 100: 14: less than 1: less than 1, respectively. These results suggest that TRK-100 is a useful tool for studying biological roles of PGI2 as well as for use as an antithrombotic agent since TRK-100 mimics its actions via specific interaction with PGI2 receptors.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP4795862	(1R)-(+)-cis-Pinane		4795-86-2	Price

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