Taprostene is a stable prostacyclin (PGI2) analog and agonist of the prostacyclin receptor, IP. It does not activate the PGE2 receptor EP4,1 which, like IP, promotes vascular smooth muscle relaxation when stimulated. Taprostene has been used extensively to study the role of the IP receptor in tissue preparations1,2 and in vivo.3,4 It has also been used in the screening and evaluation of potential IP antagonists.5
1
Jones, R.L., and Chan, K. Distinction between relaxations induced via prostanoid EP4 and IP1 receptors in pig and rabbit blood vessels. Br J Pharmacol134313-324(2001).
2
Tam, F.S.F., Chan, K., Bourreau, J., et al. The mechanisms of enhancement and inhibition of field stimulation responses of guinea-pig vas deferens by prostacyclin analogues. Br J Pharmacol1211413-1421(1997).
3
Virgolini, I., Fitscha, P., Sinzinger, H., et al. Effects of taprostene, a stable prostacyclin analogue, on haemodynamics, platelet function and arachidonate metabolism in healthy volunteers. Eur J Clin Pharmacol38347-350(1990).
4
Johnson, G., Furlan, L.E., Aoki, N., et al. Endothelium and myocardial protecting actions of taprostene, a stable prostacyclin analogue, after acute myocardial ischemia and reperfusion in cats. Circ Res661362-1370(1990).
5
Ayer, L.M., Wilson, S.M., Traves, S.L., et al. 4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxy-benzyl)-phenyl]-amine (RO1138452) is a selective, pseudo-irreversible orthosteric antagonist at the prostacyclin (IP)-receptor expressed by human airway epithelial cells: IP-receptor-mediated inhibition of CXCL9 and CXCL10 release. J Pharmacol Exp Ther324(2)815-826(2008).
Tam, F.S.F., Chan, K., Bourreau, J., et al. The mechanisms of enhancement and inhibition of field stimulation responses of guinea-pig vas deferens by prostacyclin analogues. Br J Pharmacol1211413-1421(1997).
Johnson, G., Furlan, L.E., Aoki, N., et al. Endothelium and myocardial protecting actions of taprostene, a stable prostacyclin analogue, after acute myocardial ischemia and reperfusion in cats. Circ Res661362-1370(1990).
Virgolini, I., Fitscha, P., Sinzinger, H., et al. Effects of taprostene, a stable prostacyclin analogue, on haemodynamics, platelet function and arachidonate metabolism in healthy volunteers. Eur J Clin Pharmacol38347-350(1990).
Ayer, L.M., Wilson, S.M., Traves, S.L., et al. 4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxy-benzyl)-phenyl]-amine (RO1138452) is a selective, pseudo-irreversible orthosteric antagonist at the prostacyclin (IP)-receptor expressed by human airway epithelial cells: IP-receptor-mediated inhibition of CXCL9 and CXCL10 release. J Pharmacol Exp Ther324(2)815-826(2008).
Jones, R.L., and Chan, K. Distinction between relaxations induced via prostanoid EP4 and IP1 receptors in pig and rabbit blood vessels. Br J Pharmacol134313-324(2001).