Fig. 4.
Allosteric modulation of α7L247T by A-867744, TBS-516, and TQS. Mutated α7L247T nAChRs were expressed in Xenopus oocytes and examined by two-electrode voltage-clamp recording. (A) Concentration-response data illustrating agonist activation by TBS-516 and TQS but the absence of agonist activity with A-867744. Data are the mean ± S.E.M. of three independent experiments, each from different oocytes. Data are normalized to the maximum acetylcholine response. (B) Representative traces illustrating responses to acetylcholine (10 μM; left) together with acetylcholine responses from the same oocyte after preapplication (10 seconds) and coapplication of A-867744 (1 μM; right). (C) Representative traces illustrating responses to TQS (10 μM; left) together with TQS responses from the same oocyte after preapplication (10 seconds) and coapplication of A-867744 (1 μM; right). (D) Representative traces illustrating responses to TBS-516 (10 μM; left) together with TBS-516 responses from the same oocyte after preapplication (10 seconds) and coapplication of A-867744 (1 μM; right).