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. 2023 Apr 28;68(4):135–144. doi: 10.17221/65/2022-VETMED

Table 1. Kinetic parameter values for the in vitro biotransformation of citalopram (CIT) and desmethylcitalopram (DCIT) to DCIT and didesmethyl-CIT, respectively in human and Beagle dog microsomes.

Substrate Metabolite Km1 Vmax1 IC1 Km2 Vmax2 IC2 References
Dog liver microsomes*
CIT DCIT 1.1 ± 0.3 47 ± 3 43 1 006 ± 94 591 ± 28 0.6 this study
CIT S-DCIT 1.0 ± 0.2 26 ± 1 27 848 ± 69 264 ± 10 0.3
CIT R-DCIT 1.4 ± 0.5 21 ± 2 15 1 221 ± 161 338 ± 24 0.3
DCIT DDCIT 0.6 ± 0.2 44 ± 4 73 137 ± 18 155 ± 5 1.0 this study
DCIT S-DDCIT 0.6 ± 0.1 31 ± 3 52 66 ± 11 55 ± 2 0.8
DCIT R-DDCIT 0.3 ± 0.2 11 ± 2 37 212 ± 24 105 ± 3 0.5
Human liver microsomes
CIT DCIT 174 von Moltke et al. (1999)
CIT S-DCIT 33.8 20.0 0.6 202 220 1.09 Rochat et al. (1997)
CIT R-DCIT 17.3 25.0 1.4 185 153 0.83
CIT S-DCIT 95 433 4.6 Olesen and Linnet (1999)
CIT R-DCIT 76 300 3.9
CIT S-DCIT 165 1 007 6.1 von Moltke et al. (2001)
CIT R-DCIT 256 1 254 4.9
DCIT S-DDCIT 72 95 1.3 von Moltke et al. (2001)
DCIT R-DDCIT 108 126 1.2

*Results are presented as means ± SD from six incubations carried out in duplicate

Intrisic clearence (IC) corresponds to the maximum velocity (Vmax) divided by the affinity constant, Km

IC = μl/(min × mg of protein); Km = μM; Vmax = pmol/(min × mg of protein)