Absolute quantification of imipramine and its metabolites in vivo utilizing calibrators from radiolabeled in vitro incubations. 2016

Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
Pharmaceutical Candidate Optimization, Biocon Bristol Myers-Squibb R&D Center (BBRC), Syngene International Limited, Biocon Park, Plot 2 & 3, Bommasandra IV Phase, Bangalore - 560099, India.

BACKGROUND We have demonstrated the use of a single-point calibration approach, derived from in vitro metabolite identification studies utilizing radiolabeled imipramine, that allows for the quantitation of metabolites from in vivo studies in the absence of metabolite synthetic standards. RESULTS From the in vivo study of imipramine in rats, the concentration of parent and metabolites were determined using the single-point calibration approach. Sixty seven percent of the dosed imipramine was recovered within 24 h, with 95 and 5% of drug-related material detected in feces and urine, respectively. CONCLUSIONS Using a novel single-point calibration approach from radiolabeled in vitro studies, we quantified metabolites in vivo and determined various disposition pathways.

UI MeSH Term Description Entries
D007099 Imipramine The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group. Imidobenzyle,Imizin,4,4'-Methylenebis(3-hydroxy-2-naphthoic acid)-3-(10,11-dihydro-5H-dibenzo(b,f)azepin-5-yl)-N,N-dimethyl-1-propanamine (1:2),Imipramine Hydrochloride,Imipramine Monohydrochloride,Imipramine Pamoate,Janimine,Melipramine,Norchlorimipramine,Pryleugan,Tofranil
D007553 Isotope Labeling Techniques for labeling a substance with a stable or radioactive isotope. It is not used for articles involving labeled substances unless the methods of labeling are substantively discussed. Tracers that may be labeled include chemical substances, cells, or microorganisms. Isotope Labeling, Stable,Isotope-Coded Affinity Tagging,Isotopically-Coded Affinity Tagging,Affinity Tagging, Isotope-Coded,Affinity Tagging, Isotopically-Coded,Isotope Coded Affinity Tagging,Labeling, Isotope,Labeling, Stable Isotope,Stable Isotope Labeling,Tagging, Isotope-Coded Affinity,Tagging, Isotopically-Coded Affinity
D008297 Male Males
D008862 Microsomes, Liver Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough. Liver Microsomes,Liver Microsome,Microsome, Liver
D002138 Calibration Determination, by measurement or comparison with a standard, of the correct value of each scale reading on a meter or other measuring instrument; or determination of the settings of a control device that correspond to particular values of voltage, current, frequency or other output. Calibrations
D002853 Chromatography, Liquid Chromatographic techniques in which the mobile phase is a liquid. Liquid Chromatography
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D012449 Safety Freedom from exposure to danger and protection from the occurrence or risk of injury or loss. It suggests optimal precautions in the workplace, on the street, in the home, etc., and includes personal safety as well as the safety of property. Safeties
D013058 Mass Spectrometry An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers. Mass Spectroscopy,Spectrometry, Mass,Spectroscopy, Mass,Spectrum Analysis, Mass,Analysis, Mass Spectrum,Mass Spectrum Analysis,Analyses, Mass Spectrum,Mass Spectrum Analyses,Spectrum Analyses, Mass
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats

Related Publications

Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
August 1984, The Journal of pharmacology and experimental therapeutics,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
January 2023, Methods in molecular biology (Clifton, N.J.),
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
August 1973, The Journal of pharmacy and pharmacology,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
July 2012, The Journal of molecular diagnostics : JMD,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
January 1992, NMR in biomedicine,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
June 1990, International journal of radiation oncology, biology, physics,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
January 2000, Alzheimer disease and associated disorders,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
February 1990, Cancer research,
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
November 2018, Pharmaceuticals (Basel, Switzerland),
Priyadeep Bhutani, and Devang Shah, and Ninad Varkhede, and Sandhya Mandlekar, and Silvi Chacko, and Murali Subramanian
April 1993, Radiology,
Copied contents to your clipboard!