Table 1

Metabolite profile of 0 to 72 h urine of rats and hamsters following a 30- or 2000-mg/kg oral dose of GEM1-a

Sex and Dose LevelOverall Recovery in UrineChromatographic Peaks1-b
ABCLDEFIK
Male rat
 30 mg/kg2.6390.1860.2410.1490.577 ND1-c 0.0590.2341.133ND
(29.9)(2.1)(2.7)(1.7)(6.5)(ND)(0.7)(2.7)(12.8)(ND)
 2000 mg/kg12232391-d 15123422781031318711
(53.6)(10.5)(6.6)(10.3)(1.0)(3.4)(0.4)(13.7)(8.2)(0.5)
Female rat
 30 mg/kg1.8930.0540.0640.0480.236NDND0.1721.1930.087
(32.6)(0.9)(1.1)(0.8)(4.1)(ND)(ND)(3.0)(20.5)(1.5)
 2000 mg/kg1043521-d 473644265ND225347 9
(67.7)(3.4)(3.0)(2.3)(2.9)(17.2)(ND)(14.6)(22.5)(0.6)
Male hamster
 30 mg/kg3.2300.1160.4110.0720.0110.2550.4101.2330.506ND
(90.2)(3.2)(11.5)(2.0)(0.3)(7.1)(11.5)(34.4)(14.1)(ND)
 2000 mg/kg818821-d 474112787036984 6
(83.0)(8.3)(4.8)(4.2)(1.2)(7.9)(7.1)(37.5)(8.5)(0.6)
Female hamster
 30 mg/kg3.7600.0680.3310.0430.0040.4270.1960.7681.7130.006
(90.6)(1.6)(8.0)(1.0)(0.1)(10.3)(4.7)(18.5)(41.3)(0.1)
 2000 mg/kg940821-d 3333171293541414021
(87.3)(7.7)(3.1)(3.1)(1.6)(12.0)(3.2)(38.4)(13.0)(1.9)
  • 1-a Results are expressed in milligram equivalents and percent dose excreted; percent dose in parentheses.

  • 1-b Peaks are listed in order of elution with metabolite A being the most polar. See Figs. 4 and 7 for metabolite structures.

  • 1-c Metabolite not detected.

  • 1-d Composed of at least two components. Combined results of the two are listed.