RS-61756-007: a potent and selective thromboxane receptor (TP) agonist.
The activity of RS-61756-007 (methyl-9-oxo, 15 alpha-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.
Eglen
R M
RM
Institute of Pharmacology, Syntex Research, Palo Alto, CA 94304.
Whiting
R L
RL
D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D000818:Animals; D001792:Blood Platelets / Q000187:drug effects; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011450:Prostaglandin Endoperoxides, Synthetic / Q000494:pharmacology; D011453:Prostaglandins / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011982:Receptors, Prostaglandin / Q000187:drug effects* / Q000502:physiology; D017482:Receptors, Thromboxane
D011450:Prostaglandin Endoperoxides, Synthetic; D011453:Prostaglandins; D011982:Receptors, Prostaglandin; D017482:Receptors, Thromboxane; C060701:RS 61756-007; D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid