Platelet and vascular smooth muscle thromboxane A/sup 2//prostaglandin H/sub 2/ receptors

Conference · Thu Jan 01 00:00:00 EST 1987 · Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States)

OSTI ID:6846825

Halushka, P V; Mais, D E; Saussy, Jr, D L

Thromboxane A/sub 2/ (TxA/sub 7/) and prostaglandin H/sub 2/ (PGH/sub 2/) aggregate platelets and contract vascular smooth muscle. Inasmuch as both compounds produce the same effects and presumably through the same receptor, their receptors have been referred to as TxA/sub 2//PGH/sub 2/ receptors. Pharmacological studies of stable agonists and antagonists of the TxA/sub 2//PGH/sub 2/ receptors have shown different rank order potencies for these compounds in platelets compared with blood vessels. These studies have provided evidence to support the hypothesis that the platelet TxA/sub 2//PGH/sub 2/ receptor is different from the one found in vascular tissue. The vascular receptor has been named (TxA/sub 2//PGH/sub 2/)/sub ..cap alpha../. In the past few years several radiolabeled antagonists and agonists have been developed and used in radioligand-binding studies, primarily in platelets. One of these ligands, /sup 125/I-labeled PTA-OH, a TxA/sub 2//PGH/sub 2/ receptor antagonist, has been extensively used to characterize the human platelet TxA/sub 2//PGH/sub 2/-binding site. It has been found to have a K/sub d/ of approximately 20 nM and a B/sub max/ of 2500 binding sites/platelet. Through the combination of pharmacological and biochemical approaches, it should be possible to characterize platelet and vascular TxA/sub 2//PGH/sub 2/ receptors.

• Research Organization: Medical Univ. of South Carolina, Charleston
• OSTI ID: 6846825
• Journal Information: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States), Vol. 46:1; Conference: 70. annual meeting of the Federation of American Societies for Experimental Biology, St. Louis, MO, USA, 15 Apr 1986
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
BLOOD PLATELETS
BLOOD COAGULATION
MUSCLES
CONTRACTION
PROSTAGLANDINS
BIOCHEMICAL REACTION KINETICS
RECEPTORS
IODINE 125
TRACER TECHNIQUES
BETA DECAY RADIOISOTOPES
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BODY FLUIDS
DAYS LIVING RADIOISOTOPES
ELECTRON CAPTURE RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
IODINE ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
MATERIALS
MEMBRANE PROTEINS
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
PROTEINS
RADIOISOTOPES
REACTION KINETICS
550201* - Biochemistry- Tracer Techniques