Document Detail


Disposition of 2-mercaptobenzothiazole and 2-mercaptobenzothiazole disulfide in rats dosed intravenously, orally, and topically and in guinea pigs dosed topically.
MedLine Citation:
PMID:  2724369     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
To determine the metabolic disposition of [14C]-2-mercaptobenzothiazole (MBT) and [14C]-2-mercaptobenzothiazole disulfide (MBTS), male and female rats were dosed topically. Topical doses were 36.1 micrograms/animal for [14C]MBT and 33.6 micrograms/animal for [14C]MBTS. Although more MBT passed through the skin than MBTS and although, relative to rats, guinea pigs absorbed a greater percentage of the dose (33.4% compared to 16.1-17.5% of the MBT and 12.2% compared to 5.94-7.87% for MBTS), the disposition of radioactivity derived from the two compounds was similar. Washing of the skin removed more of the radioactivity from guinea pigs than from rats. For both sexes of rats dosed intravenously with [14C]MBT (0.602 mg/kg) or [14C]MBTS (0.571 mg/kg), disposition of the compounds was similar. In 72 h, 90.9-101% of the dose appeared in the urine and 3.79-15.1% in the feces. At this time, a small portion of the administered radioactivity (1.52-1.96% of the dose) remained associated with erythrocytes. Oral dosing of rats for 14 d with unlabeled MBT (0.510 mg/kg.d) prior to a single dose of [14C]MBT (0.503 mg/kg) or with unlabeled MBTS (0.521 mg/kg.d) prior to a single dose of [14C]MBTS (0.730 mg/kg). For both sexes, disposition of the compounds was similar. At 96 h after dosing, a small portion of the administered radioactivity (1.20-1.69% of the dose) remained associated with erythrocytes, most of which was bound to the membranes. For both compounds and sexes, 60.8-101% of the radioactivity administered appeared in the urine and 3.46-9.99% in the feces in 96 h. At the time, only trace amounts of radioactivity remained in tissues other than blood. Of these tissues, thyroid contained the highest concentration. In the urine, there was a detectable MBT or MBTS, but there were two metabolites, one of which was identified as a thioglucuronide derivative of MBT. The other was possibly a sulfonic acid derivative of MBT. In conclusion, there were similarities in absorption, distribution, and metabolism of [14C]MBT and [14C]MBTS in rats and in guinea pigs, indicating that [14C]MBTS was readily converted to [14C]MBT.
Authors:
S M el Dareer; J R Kalin; K F Tillery; D L Hill; J W Barnett
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of toxicology and environmental health     Volume:  27     ISSN:  0098-4108     ISO Abbreviation:  J Toxicol Environ Health     Publication Date:  1989  
Date Detail:
Created Date:  1989-06-23     Completed Date:  1989-06-23     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7513622     Medline TA:  J Toxicol Environ Health     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  65-84     Citation Subset:  IM    
Affiliation:
Southern Research Institute, Birmingham, Alabama 35255-3505.
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MeSH Terms
Descriptor/Qualifier:
Absorption
Administration, Oral
Administration, Topical
Animals
Benzothiazoles
Carbon Radioisotopes / diagnostic use
Environmental Exposure
Female
Guinea Pigs
Injections, Intravenous
Male
Rats
Rats, Inbred F344
Thiazoles / administration & dosage,  metabolism,  pharmacokinetics*
Tissue Distribution
Chemical
Reg. No./Substance:
0/Benzothiazoles; 0/Carbon Radioisotopes; 0/Thiazoles; 120-78-5/dibenzothiazyl disulfide; 149-30-4/captax

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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