Figure 1.

In vitro pharmacological properties of A-582941. A, Structure of A-582941. B, Displacement of [³H]A-585539 and [³H]cytisine binding to rat brain membranes by A-582941. C, Current traces showing activation of human α7 nAChRs expressed in Xenopus oocytes by ACh (top) and A-582941 (bottom). After preincubation with methyllycaconitine (MLA; 10 nm, 5 min), current responses to both A-582941 and ACh were abolished. Responses returned to control levels on washout. D, Concentration–response data (mean ± SEM) are shown for A-582941 as agonist at human and rat α7 nAChR expressed in Xenopus oocytes. The EC₅₀ and percentage maximal efficacy values are summarized in Results.