Abstract
CMT-3 is a NON-ANTIMICROBIAL tetracycline (TC), chemically modified to enhance its collagenase-inhibitory property. This property is therapeutically useful in treating diseases such as periodontitis, cancer and arthritis. CMT-3 was labeled with tritium ( 3 H) at Carbon 7. Four adult male Sprague-Dawley rats (350-400 g body weight) were gavaged once with a mixture of cold CMT-3 and ( 3 H) CMT-3 (750 mu Ci). An additional four rats were gavaged for 2 days with cold CMT-3(15 mg/Kg/day) and on the third day the rats were gavaged with a mixture of cold and (3 H) CMT-3 (750 mu Ci) and all 8 rats were placed in the metabolic cages. Blood samples were collected from the tail at multiple intervals from 1-14 hr after ( 3 H) CMT-3 administration. At 14 hr, the rats were anesthetized, euthanized and various tissues including visceral organs were removed and weighed. The contents of GI tracts were emptied and added to the fecal pellets and weighed. The urine samples were collected and volume measured. Each tissue or organ was minced finely with scissors and 100 mg of tissue was digested in 1 ml of Tissue-solv (Packard Lab), for 4 hrs at 37 o C and each sample was diluted up to 10 ml of distilled water. A 100 ml aliquot was taken and diluted with an equal volume of glacial acetic acid, 10 ml of Atom-lite was added and counted for radioactivity in a liquid scintillation spectrometer. This biodistribution study revealed that over 14 hrs, 54 percent and 3 percentof ( 3 H) CMT-3 were excreted in the feces and urine, respectively. The serum ( 3 H) CMT-3 count reached its maximum value at about 12 hours. The tissues retained the CMTs as follow: muscle (23percent); skin (2.41percent); bone (1.72percent); and the brain retained 0.21percent of the label. The radioactive CMT-3 in the visceral organs is as follows: GI tract - its contents (8.9percent); heart (0.41percent), testis (0.41percent); lungs greater than(0.16percent); spleen (0.08percent); liver (0.03percent); kidneys greater than (0.02percent).
Keywords: Radiolabeled CMT 3, Non antimicrobial tetracycline, experimental peridontitis, pharmacokinetics studies, CMT 3 administratio
Current Medicinal Chemistry
Title: Biodistribution of Radiolabeled [ 3 H] CMT-3 in Rats
Volume: 8 Issue: 3
Author(s): J. Chen, M. Bookbinder, M. E. Ryan, L. M. Golub, R. Ashley and N. S. Ramamurthy
Affiliation:
Keywords: Radiolabeled CMT 3, Non antimicrobial tetracycline, experimental peridontitis, pharmacokinetics studies, CMT 3 administratio
Abstract: CMT-3 is a NON-ANTIMICROBIAL tetracycline (TC), chemically modified to enhance its collagenase-inhibitory property. This property is therapeutically useful in treating diseases such as periodontitis, cancer and arthritis. CMT-3 was labeled with tritium ( 3 H) at Carbon 7. Four adult male Sprague-Dawley rats (350-400 g body weight) were gavaged once with a mixture of cold CMT-3 and ( 3 H) CMT-3 (750 mu Ci). An additional four rats were gavaged for 2 days with cold CMT-3(15 mg/Kg/day) and on the third day the rats were gavaged with a mixture of cold and (3 H) CMT-3 (750 mu Ci) and all 8 rats were placed in the metabolic cages. Blood samples were collected from the tail at multiple intervals from 1-14 hr after ( 3 H) CMT-3 administration. At 14 hr, the rats were anesthetized, euthanized and various tissues including visceral organs were removed and weighed. The contents of GI tracts were emptied and added to the fecal pellets and weighed. The urine samples were collected and volume measured. Each tissue or organ was minced finely with scissors and 100 mg of tissue was digested in 1 ml of Tissue-solv (Packard Lab), for 4 hrs at 37 o C and each sample was diluted up to 10 ml of distilled water. A 100 ml aliquot was taken and diluted with an equal volume of glacial acetic acid, 10 ml of Atom-lite was added and counted for radioactivity in a liquid scintillation spectrometer. This biodistribution study revealed that over 14 hrs, 54 percent and 3 percentof ( 3 H) CMT-3 were excreted in the feces and urine, respectively. The serum ( 3 H) CMT-3 count reached its maximum value at about 12 hours. The tissues retained the CMTs as follow: muscle (23percent); skin (2.41percent); bone (1.72percent); and the brain retained 0.21percent of the label. The radioactive CMT-3 in the visceral organs is as follows: GI tract - its contents (8.9percent); heart (0.41percent), testis (0.41percent); lungs greater than(0.16percent); spleen (0.08percent); liver (0.03percent); kidneys greater than (0.02percent).
Export Options
About this article
Cite this article as:
Chen J., Bookbinder M., Ryan E. M., Golub M. L., Ashley R. and Ramamurthy S. N., Biodistribution of Radiolabeled [ 3 H] CMT-3 in Rats, Current Medicinal Chemistry 2001; 8 (3) . https://dx.doi.org/10.2174/0929867013373615
DOI https://dx.doi.org/10.2174/0929867013373615 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Antiproliferative Properties of 7,8-Ethylene Diamine Chelator-Lipophilic Fluoroquinolone
Derivatives Against Colorectal Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Recent Developments in Collagen Patents
Recent Patents on Regenerative Medicine Endotoxin, TLR4 Signaling and Vascular Inflammation: Potential Therapeutic Targets in Cardiovascular Disease
Current Pharmaceutical Design Bone Regeneration with Biomaterials and Active Molecules Delivery
Current Pharmaceutical Biotechnology Formulation and Investigation of a Lipid Based Delivery System Containing Antimicrobials for the Treatment of Periodontal Disease
Current Drug Delivery Mucoadhesive Buccal Systems as a Novel Strategy for Anti-Inflammatory Drugs Administration
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Formulation of Chitosan Nanoparticles Loaded with Metronidazole for the Treatment of Infectious Diseases
Letters in Drug Design & Discovery Antimicrobial Peptides: Mediators of Innate Immunity as Templates for the Development of Novel Anti-Infective and Immune Therapeutics
Current Pharmaceutical Design A Pulmonary Perspective on GASPIDs: Granule-Associated Serine Peptidases of Immune Defense
Current Respiratory Medicine Reviews Editorial (Thematic Issue: Nanotechnology for Drug Delivery: Part I)
Current Pharmaceutical Design Promising Alternative Therapeutics for Oral Candidiasis
Current Medicinal Chemistry Prognostic and Predictive Value of Epithelial to Mesenchymal Transitionassociated Markers in Oral Squamous Cell Carcinoma
Current Proteomics Nanoplatforms for Promoting Osteogenesis in Ovariectomy-Induced Osteoporosis in the Experimental Model
Current Nanomedicine Edible Transgenic Plant Vaccines for Different Diseases
Current Pharmaceutical Biotechnology Formulation and Characterisation of Tetracycline-Containing Bioadhesive Polymer Networks Designed for the Treatment of Periodontal Disease
Current Drug Delivery Medicinal Properties of Neem Leaves: A Review
Current Medicinal Chemistry - Anti-Cancer Agents Updated Acute Community-Acquired Pneumonia in Adults: Guidelines for Initial Antimicrobial Therapy Based on Local Evidence from the South American Working Group (Consensur II)
Current Respiratory Medicine Reviews Investigation of Methylene Blue Release from Functional Polymeric Systems Using Dielectric Analysis
Current Drug Delivery Recent Patents on Stimuli Responsive Hydrogel Drug Delivery System
Recent Patents on Drug Delivery & Formulation Biodegradable Composite Scaffolds: A Strategy to Modulate Stem Cell Behaviour
Recent Patents on Drug Delivery & Formulation