Enzyme immunoassay for 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl)benzimidazole, a novel 5-HT3 receptor antagonist.
An enzyme immunoassay (EIA) has been developed for determination of 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl) benzimidazole (KB-6806), a novel 5-HT3 receptor antagonist. Anti-KB-6806 antiserum was elicited against the KB-6806-bovine serum albumin (BSA) conjugate prepared by a diazo coupling reaction through the inherent 6-amino group. Beta-galactosidase-labeled 6-amino-5-chloro-1-isobutyl-2-(4-methyl-1-piperazinyl)benzimidazole was similarly prepared by diazo coupling reaction as an enzyme-labeled antigen with a hapten heterologous combination of antiserum. The modification at the 4-methyl group of the piperazine moiety of KB-6806 significantly decreased the binding affinity to the antibody. This method could quantitate KB-6806 in dog plasma in the concentration range of 0.078-10 ng/ml with good accuracy and precision. The EIA method has been successfully applied to the determination of KB-6806 in plasma after intravenous administration of KB-6806 to dogs.
Fujikawa
M
M
Research & Development Division, Nippon Organon K. K., Osaka, Japan. Fujikawa.Masaaki@organon.co.jp
Teratani
F
F
Nakada
Y
Y
D000818:Animals; D000918:Antibody Specificity; D019540:Area Under Curve; D001562:Benzimidazoles / Q000032:analysis*; D002138:Calibration; D003429:Cross Reactions; D004285:Dogs; D006241:Haptens / Q000276:immunology; D007124:Immunoenzyme Techniques; D008297:Male; D011985:Receptors, Serotonin / Q000187:drug effects*; D044406:Receptors, Serotonin, 5-HT3; D015203:Reproducibility of Results; D012702:Serotonin Antagonists / Q000032:analysis* / Q000097:blood / Q000493:pharmacokinetics; D012710:Serum Albumin, Bovine / Q000276:immunology; D001616:beta-Galactosidase / Q000276:immunology
D001562:Benzimidazoles; D006241:Haptens; C121292:KB R6933; D011985:Receptors, Serotonin; D044406:Receptors, Serotonin, 5-HT3; D012702:Serotonin Antagonists; D012710:Serum Albumin, Bovine; D001616:beta-Galactosidase