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Biologic stability of tauro-23-(/sup 75/Se) selena-25-homocholic acid

Journal Article · · J. Nucl. Med.; (United States)
OSTI ID:6924283
The stability of tauro-23-(/sup 75/Se)selena-25-homocholic acid (SeHCAT) towards deconjugation by the enzyme cholylglycine hydrolase was compared with that of taurocholate: whereas taurocholate underwent 58% deconjugation within 2 hr, SeHCAT suffered only 8% deconjugation plus 5% conversion to an unknown product within 24 hr. Incubation of SeHCAT under anaerobic conditions for 48 hr at 37 degrees C with human fecal organisms resulted in considerable deconjugation, 7 alpha-dehydroxylation, and dehydrogenation. Twenty-four hours after the simultaneous administration of SeHCAT and tauro-(24-/sup 14/C)cholate to a rabbit the recovery of /sup 75/Se in bile was 90% of that of /sup 14/C. Forty-eight hours following administration of SeHCAT to a second rabbit residual bile radioactivity revealed 80% deconjugation and dehydroxylation and 60% reconjugation with glycine. Although SeHCAT is more resistant than taurocholate towards modification by fecal bacterial enzymes, within the rabbit it follows the principal metabolic pathways of the natural bile acids.
Research Organization:
Amersham International Plc, Bucks (England)
OSTI ID:
6924283
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 29:8; ISSN JNMEA
Country of Publication:
United States
Language:
English