SQ 29,548 is a highly selective TP receptor antagonist which binds to the human recombinant TP receptor with a Ki of 4.1 nM.1 It inhibits the aggregation of washed human platelets induced by U-46619 with an IC50 of 0.06 µM.2 It antagonizes U-46619 induced contraction of rat and guinea pig tracheal, arterial, and venous smooth muscles with drug/receptor dissociation constants (KB) in the range of 0.5-1.7 nM.3 SQ 29,548 also inhibits the contraction of rat vascular smooth muscle induced by 8-iso PGF2α.4
1
Abramovitz, M., Adam, M., Boie, Y., et al. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta1483285-293(2000).
2
Ogletree, M.L., Harris, D.N., Greenberg, R., et al. Pharmacological actions of SQ 29,548, a novel selective thromboxane antagonist. J Pharmacol Exp Ther234435-441(1985).
3
Ogletree, M.L., and Allen, G.T. Interspecies differences in thromboxane receptors: Studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. J Pharmacol Exp Ther260789-794(1992).
4
Fukunaga, M., Makita, N., Roberts, L.J., et al. Evidence for the existence of F2-isoprostane receptors on rat vascular smooth muscle cells. Am J Physiol264C1619-C1624(1993).
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OC(=O)CCC/C=C\CC1C2CCC(O2)C1CNNC(=O)Nc1ccccc1
Background Reading
Fukunaga, M., Makita, N., Roberts, L.J., et al. Evidence for the existence of F2-isoprostane receptors on rat vascular smooth muscle cells. Am J Physiol264C1619-C1624(1993).
Ogletree, M.L., and Allen, G.T. Interspecies differences in thromboxane receptors: Studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. J Pharmacol Exp Ther260789-794(1992).
Komiotis, D., Lim, C.T., Dieter, J.P., et al. PGH2 analogs as potential antiplatelet derivatives. J Med Chem353033-3039(1992).
Ogletree, M.L., Harris, D.N., Greenberg, R., et al. Pharmacological actions of SQ 29,548, a novel selective thromboxane antagonist. J Pharmacol Exp Ther234435-441(1985).