Description
ST-034307 (133406-29-8) is anovel selective adenylyl cyclase 1 (AC1) inhibitor, IC50=2.3 μM . Inhibits calcium2+-stimulated cAMP accumulation in HEK cells stably transfected with AC11. It was also shown to inhibit AC1 stimulated by forskolin- and Gαs-coupled receptors in HEK-AC1 cells. It enhanced μ-opioid receptor-mediated inhibition of AC1 but it blocked heterologous sensitization of AC1 caused by chronic μ-opioid receptor activation.1,3Displays analgesic properties in a mouse model of inflammatory pain.1A useful tool for exploring the involvement of AC1 in cellular signalling.2
References
[1] TARSIS F. BRUST. Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties[J]. Science Signaling, 2017, 10 467. DOI:
10.1126/scisignal.aah5381[2] ZHENG JIANG. Cyclic-Nucleotide- and HCN-Channel-Mediated Phototransduction in Intrinsically Photosensitive Retinal Ganglion Cells.[J]. Journal of Chemical Theory and Computation, 2018: 652-664.e12. DOI:
10.1016/j.cell.2018.08.055[3] WATTS V J. Selective Adenylyl Cyclase Type 1 Inhibitors as Potential Opioid Alternatives For Chronic Pain[J]. Neuropsychopharmacology, 2017, 43 1: 215-216. DOI:
10.1038/npp.2017.190