Metabolic fate of indeloxazine hydrochloride: alpha-glucoside formation in rats.
1. After oral administration of indeloxazine hydrochloride ((+/-)-2-[(inden-7-yloxy)methyl]morpholine hydrochloride) to rats, two conjugates, which were labile to alpha-glucosidase hydrolysis but refractory to beta-glucosidase, were isolated from the urine. 2. Mass spectral and n.m.r. analyses confirmed that these conjugates were alpha-D-glucopyranosides of M-2 (trans-4-(2-morpholinylmethoxy)-1,2-indandiol) and M-3 (trans-6-[[(1,2-dihydroxy-4-indanyl)oxy]-methyl]-3-morpholinone). 3. These are probably the first examples of foreign compounds conjugated with glucose in the alpha-configuration.
Kamimura
H
H
Drug Metabolism Department, Yamanouchi Pharmaceutical Co., Ltd, Tokyo, Japan.
Kawai
R
R
Kudo
H
H
D000818:Animals; D005960:Glucosides / Q000096:biosynthesis* / Q000652:urine; D006027:Glycosides / Q000096:biosynthesis*; D006868:Hydrolysis; D008297:Male; D009025:Morpholines / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains; D000520:alpha-Glucosidases / Q000378:metabolism
D005960:Glucosides; D006027:Glycosides; D009025:Morpholines; C020852:indeloxazine; D000520:alpha-Glucosidases