Use of antisera in the isolation of human specific conjugates of haloperidol

Xenobiotica. 1989 Jul;19(7):781-93. doi: 10.3109/00498258909042315.


1. Three conjugated metabolites of haloperidol were isolated from urine of patients on haloperidol and purified by h.p.l.c. with immunological detection, using three types of anti-haloperidol antisera. 2. Structures of the metabolites were: a sulphate conjugate of the 2-hydroxylated 4-fluorophenyl ring of reduced haloperidol (MH-1), a glucuronide conjugate at the same position as MH-1 (MH-2), and a glucuronide conjugate of the hydroxy group of haloperidol (MH-3). 3. MH-3 was the main urinary metabolite in volunteers receiving haloperidol, who excreted 18% of the dose in the 24 h urine as MH-3, while other conjugates were less than 1%. MH-3 could not be hydrolysed with beta-glucuronidase, due to steric hindrance. 4. Immunological detection of conjugated metabolites is very useful in metabolic studies in humans because of its sensitivity and specificity.

MeSH terms

  • Adult
  • Biotransformation
  • Chromatography, High Pressure Liquid
  • Cross Reactions
  • Female
  • Haloperidol / immunology
  • Haloperidol / isolation & purification*
  • Haloperidol / metabolism
  • Humans
  • Male
  • Middle Aged
  • Radioimmunoassay
  • Spectrophotometry, Ultraviolet


  • Haloperidol