Adenylyl cyclase 1 (AC1) inhibitor (IC50
= 2.3 μM). Exhibits some selectivity for AC1 over other AC isoforms, with no significant activity against AC8. Inhibits Ca2+
/calmodulin-stimulated cAMP accumulation in hippocampal homogenates. Enhances μ opioid receptor (MOR)-mediated inhibition of AC1 in cellular assays and inhibits development and maintenance of MOR-mediated sensitization of AC1. Active in vivo
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Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties.
Brust et al.