Description
ST-034307 (133406-29-8) is a?novel 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.1,3?Displays analgesic properties in a mouse model of inflammatory pain.1?A useful tool for exploring the involvement of AC1 in cellular signalling.2
References
1) Brust?et al.?(2017),?Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties; Sci. Signal,?10?eaah5381
2) Jiang?et al,?(2018),?Cyclic-Nucleotide- and HCN-Channel-Mediated Phototransduction in Intrinsically Photosensitive Retinal Ganglion Cells;. Cell?175?652
3) Watts (2018),?Selective Adenylyl Cyclase Type 1 Inhibitors as Potential Opioid Alternatives For Chronic Pain;?Neuropsychopharmacology?43?215
