Fig. 4.

N-1,2-Diol analogs inhibit [³H]DTBZ binding to vesicle membranes from rat whole brain preparations. For clarity of presentation, compounds are grouped according to structural similarity of additions to the phenyl rings: standards, lobeline, lobelane, and N-1,2-diol analogs (top left), N-1,2-diol analogs containing 1-naphthyl or 4-biphenyl substituents (top right), N-1,2-diol analogs containing aromatic methoxy or methylenedioxy substituents (bottom left), or N-1,2-diol analogs containing aromatic halogeno substituents (bottom right). Nonspecific [³H]DTBZ binding was determined in the presence of 10 μM Ro-4-1284. Control (CON) represents specific [³H]DTBZ binding in the absence of analog (1.65 ± 0.05 pmol/mg protein). Symbol inset shows compounds in order from highest to lowest affinity. n = 4 rats/analog. Previous results for lobeline and lobelane were obtained from Nickell et al., 2010.