Table 2. Affinity for the Human H3R of Photoswitchable Azobenzene-Derived H3R Ligands.
Photostationary state area percentages after illumination with 360 ± 20 nm at 1 mM in DMSO-d6 and as determined by LCMS analysis at 254 nm.
Measured by displacement of [3H]-Nα-methylhistamine on HEK293T cell homogenates transiently expressing the H3R.
Defined as pKi PSS cis – pKitrans.
Unsubstituted phenyl.
Trans sample contained 3.9 area % cis compound.