TABLE 2

In vitro cytochrome P450 metabolism of H3 antagonists

Compound
Calculated fu(inc)
HLM Clint,un
RLM Clint,un
μl/min/mg protein
1 0.58 <7 27
2 0.44 <7 19
3 0.89 <7 20
4 N.A. <7 <7
5 N.A. <7 <7
6 N.A. <7 <7
7 N.A. <7 <7
8 N.A. <7 <7
9 N.A. <7 <7
10 N.A. <7 <7
11 N.A. <7 <7
12 N.A. <7 <7
13 N.A. <7 <7
14 N.A. <7 <7
15 N.A. <7 <7
16
N.A.
<7
<7

  • HLM, human liver microsomes; RLM, rat liver microsomes; Clint,un, unbound intrinsic clearance; N.A., not applicable.