Fig. 1

Saturation binding curve (a) and Scatchard plot (b) for ³H-THK5117 (0.04-270 nM) in temporal lobe brain homogenates from four patients with AD. The solid regression line was determined by GraphPad Prism software and corresponds to the low affinity site. The dotted regression line was determined manually and corresponds to the high affinity site. The corresponding Kd and Bmax values are given below the curve. (c) Competition binding curve between THK5117 (10⁻¹³-10⁻⁵ M) and ³H-THK5117 (3 nM) in temporal lobe brain homogenates from four patients with AD. Analyses from non-linear regression using a least square ordinary fit in GraphPad Prism software showed three binding sites. Ki: inhibitory constant. r² = regression coefficient