RS‐61756‐007: a potent and selective thromboxane receptor (TP) agonist

The activity of RS‐61756‐007 (methyl‐9‐oxo, 15 α‐hydroxy, 16‐phenoxy, 17,18,19,20‐tetranor prosta 4,5,13(E)trienoate, 4,5,6 (R), 8(R)) has been assessed at prostanoid receptors (DP, EP1, EP2, FP, IP and TP) in‐vitro. The activity profile of RS‐61756‐007 resembles that of U46619, in that agonism was observed at TP and to a lesser extent at FP receptors, but there was no activity at the remaining subtypes. The actions of both RS‐61756‐007 and U46619 were antagonized in a similar manner by the TP antagonist SQ 29,548. We conclude that RS‐61756‐007 is a highly potent TP agonist.

[1]  R. Eglen,et al.  The action of prostanoid receptor agonists and antagonists on smooth muscle and platelets , 1988, British journal of pharmacology.

[2]  B. Whittle,et al.  Prostaglandin D2 interacts at thromboxane receptor‐sites on guinea‐pig platelets , 1986, British journal of pharmacology.

[3]  R. A. Coleman,et al.  AH23848: a thromboxane receptor-blocking drug that can clarify the pathophysiologic role of thromboxane A2. , 1985, Circulation.

[4]  M. Ogletree,et al.  Pharmacological actions of SQ 29,548, a novel selective thromboxane antagonist. , 1985, The Journal of pharmacology and experimental therapeutics.

[5]  B. Whittle,et al.  Interaction of prostaglandin D2 with prostacyclin, carbacyclin and the hydantoin prostaglandin, BW245C, in guinea‐pig platelets , 1985, British journal of pharmacology.

[6]  F. H. Schmidt,et al.  The pharmacological profile of the thromboxane A2 antagonist BM 13.177. A new anti-platelet and anti-thrombotic drug. , 1984, Thrombosis research.

[7]  R. A. Coleman,et al.  Studies on the characterisation of prostanoid receptors: a proposed classification. , 1982, Prostaglandins.

[8]  R. L. Jones,et al.  ANTAGONISM OF THE THROMBOXANE‐SENSITIVE CONTRACTILE SYSTEMS OF THE RABBIT AORTA, DOG SAPHENOUS VEIN AND GUINEA‐PIG TRACHEA , 1982, British journal of pharmacology.

[9]  Yang Dong,et al.  EFFECTS OF PROSTAGLANDINS AND THROMBOXANE ANALOGUES ON BULLOCK AND DOG IRIS SPHINCTER PREPARATIONS , 1982, British journal of pharmacology.

[10]  R. A. Coleman,et al.  COMPARISON OF THE ACTIONS OF U‐46619, A PROSTAGLANDIN H2‐ANALOGUE, WITH THOSE OF PROSTAGLANDIN H2 AND THROMBOXANE A2 ON SOME ISOLATED SMOOTH MUSCLE PREPARATIONS , 1981, British journal of pharmacology.

[11]  J. Emmerson,et al.  The zig‐zag tracheal strip , 1979, The Journal of pharmacy and pharmacology.

[12]  E. Horton,et al.  A COMPARISON OF THE ACTIONS OF PROSTAGLANDINS F2a AND E1 ON SMOOTH MUSCLE , 1965 .

[13]  E. Horton,et al.  A COMPARISON OF THE ACTIONS OF PROSTAGLANDINS F2-ALPHA AND E1 ON SMOOTH MUSCLE. , 1965, British journal of pharmacology and chemotherapy.

[14]  H. Schild,et al.  SOME QUANTITATIVE USES OF DRUG ANTAGONISTS , 1997, British journal of pharmacology and chemotherapy.

[15]  R. Furchgott,et al.  Reactions of strips of rabbit aorta to epinephrine, isopropylarterenol, sodium nitrite and other drugs. , 1953, The Journal of pharmacology and experimental therapeutics.