Skip to main content
. 2008 Dec 19;328(3):976–981. doi: 10.1124/jpet.108.145458

TABLE 2.

In vivo antagonism potencies and in vitro receptor binding affinities of MDL100907

MDL100907 Ketanserin Ritanserin
In vivo antagonism
    DOM discriminative stimulus (pA2, mg/kg) 0.0006a (0.0003-0.0012) 0.0075a (0.0053-0.0157) 0.0102a (0.0071-0.0158)
    (±)-1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane -induced head twitch (ED50, mg/kg) 0.005b 0.029c (0.009-0.096) 0.027c (0.008-0.091)
In vitro binding
    5-HT2A receptor (Ki, nM) 0.85d 3.16c 3.80c
    5-HT2C receptor (Ki, nM) 88d 186c 2.3c
    α1 Adrenergic (Ki, nM) 128d 15c 190c
a

Potency (milligrams per kilogram) to antagonize the DOM discriminative stimulus in monkeys (values in parentheses are the 95% confidence limits).

b

ED50 recalculated from Vickers et al. (2001).

c

From Kleven et al. (1997) (values in parentheses are 95% confidence limits).

d

From Kehne et al. (1996).