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Title: Disposition of 2-mercaptobenzothiazole and 2-mercaptobenzothiazole disulfide in rats dosed intravenously, orally, and topically and in guinea pigs dosed topically

Abstract

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 or (14C)MBTS, 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 remained associated with erythrocytes. Oral dosing of rats for 14 d with unlabeled MBT prior to a single dose of (14C)MBT or with unlabeled MBTS 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 remained associated with erythrocytes, most of which wasmore » 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.« less

Authors:
; ; ; ;  [1]
  1. Southern Research Institute, Birmingham, AL (USA)
Publication Date:
OSTI Identifier:
5404442
Resource Type:
Journal Article
Journal Name:
Journal of Toxicology and Environmental Health; (USA)
Additional Journal Information:
Journal Volume: 27:1; Journal ID: ISSN 0098-4108
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; THIAZOLES; METABOLISM; CARBON 14 COMPOUNDS; ENVIRONMENTAL EXPOSURE; GUINEA PIGS; INTRAVENOUS INJECTION; LABELLED COMPOUNDS; ORAL ADMINISTRATION; RATS; SKIN ABSORPTION; TISSUE DISTRIBUTION; TRACER TECHNIQUES; ABSORPTION; ANIMALS; AZOLES; DISTRIBUTION; HETEROCYCLIC COMPOUNDS; INJECTION; INTAKE; ISOTOPE APPLICATIONS; MAMMALS; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC SULFUR COMPOUNDS; RODENTS; UPTAKE; VERTEBRATES; 550501* - Metabolism- Tracer Techniques

Citation Formats

el Dareer, S M, Kalin, J R, Tillery, K F, Hill, D L, and Barnett, Jr, J W. Disposition of 2-mercaptobenzothiazole and 2-mercaptobenzothiazole disulfide in rats dosed intravenously, orally, and topically and in guinea pigs dosed topically. United States: N. p., 1989. Web. doi:10.1080/15287398909531279.
el Dareer, S M, Kalin, J R, Tillery, K F, Hill, D L, & Barnett, Jr, J W. Disposition of 2-mercaptobenzothiazole and 2-mercaptobenzothiazole disulfide in rats dosed intravenously, orally, and topically and in guinea pigs dosed topically. United States. https://doi.org/10.1080/15287398909531279
el Dareer, S M, Kalin, J R, Tillery, K F, Hill, D L, and Barnett, Jr, J W. 1989. "Disposition of 2-mercaptobenzothiazole and 2-mercaptobenzothiazole disulfide in rats dosed intravenously, orally, and topically and in guinea pigs dosed topically". United States. https://doi.org/10.1080/15287398909531279.
@article{osti_5404442,
title = {Disposition of 2-mercaptobenzothiazole and 2-mercaptobenzothiazole disulfide in rats dosed intravenously, orally, and topically and in guinea pigs dosed topically},
author = {el Dareer, S M and Kalin, J R and Tillery, K F and Hill, D L and Barnett, Jr, J W},
abstractNote = {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 or (14C)MBTS, 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 remained associated with erythrocytes. Oral dosing of rats for 14 d with unlabeled MBT prior to a single dose of (14C)MBT or with unlabeled MBTS 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 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.},
doi = {10.1080/15287398909531279},
url = {https://www.osti.gov/biblio/5404442}, journal = {Journal of Toxicology and Environmental Health; (USA)},
issn = {0098-4108},
number = ,
volume = 27:1,
place = {United States},
year = {Sun Jan 01 00:00:00 EST 1989},
month = {Sun Jan 01 00:00:00 EST 1989}
}