Description
SQ 22,536 is an inhibitor of adenylyl cyclase with an IC
50 value of 13 μM for inhibition of prostaglandin E
1-
stimulated increase in cAMP in intact platelets. It has been used to evaluate adenylyl cyclase activity during iloprost-
induced vasorelaxation of isolated pulmonary veins or aorta in several research paradigms, inhibiting cAMP elevation at concentrations of 100-
300 μM without effecting relaxation.
Uses
SQ 22,536 was used to study the role of adenylate cyclase in differentiation of PC12 cells and in gap junctional intercellular communication in breast cancer cells.
Definition
ChEBI: A nucleoside analogue that is adenine in which the nitrogen at position 9 has been substituted by a tetrahydrofuran-2-yl group. It is an adenylate cyclase inhibitor.
Biological Activity
Inhibitor of adenylyl cyclase (IC 50 = 1.4 μ M). Inhibits PGE 1 -stimulated increases in cAMP levels in intact human platelets.
Biochem/physiol Actions
SQ 22,536 is an effective inhibitor of not only basal but also prosptaglandin E1-activated adenylate cyclase activities in platelets.1 It reverses hyperalgesia contralaterally and ipsilaterally when injected intramuscularly in rats.2
References
[1] R J HASLAM J V D M M Davidson. Inhibition of adenylate cyclase by adenosine analogues in preparations of broken and intact human platelets. Evidence for the unidirectional control of platelet function by cyclic AMP.[J]. Biochemical Journal, 1978, 176 1: 83-95. DOI:
10.1042/bj1760083[2] SALLY TURCATO Lucie H C. Effects of the adenylyl cyclase inhibitor SQ22536 on iloprost-induced vasorelaxation and cyclic AMP elevation in isolated guinea-pig aorta[J]. British Journal of Pharmacology, 2009, 126 4: 845-847. DOI:
10.1038/sj.bjp.0702383[3] YUANSHENG GAO J U R. Effects of SQ 22536, an adenylyl cyclase inhibitor, on isoproterenol-induced cyclic AMP elevation and relaxation in newborn ovine pulmonary veins[J]. European journal of pharmacology, 2002, 436 3: Pages 227-233. DOI:
10.1016/s0014-2999(02)01261-x
