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Xenobiotica
the fate of foreign compounds in biological systems
Volume 22, 1992 - Issue 7
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Research Article

Metabolism of calcium antagonist Ro 40-5967: a case history of the use of diode-array u.v. spectroscopy and thermospray-mass spectrometry in the elucidation of a complex metabolic pathway

H. R. Wiltshire Department of Pharmacokinetics and Metabolism, Roche Products Ltd., PO Box 8, Welwyn Garden City, Herts, AL7 3AY, UK
,
S. R. Harris Department of Pharmacokinetics and Metabolism, Roche Products Ltd., PO Box 8, Welwyn Garden City, Herts, AL7 3AY, UK
,
K. J. Prior Department of Pharmacokinetics and Metabolism, Roche Products Ltd., PO Box 8, Welwyn Garden City, Herts, AL7 3AY, UK
,
U. M. Kozlowski Department of Pharmacokinetics and Metabolism, Roche Products Ltd., PO Box 8, Welwyn Garden City, Herts, AL7 3AY, UK
&
E. Worth Department of Pharmacokinetics and Metabolism, Roche Products Ltd., PO Box 8, Welwyn Garden City, Herts, AL7 3AY, UK
Pages 837-857 | Received 19 Jun 1991, Accepted 20 Jan 1992, Published online: 22 Sep 2008

Citations (14)

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Sylvie I Ertel & Jean-Paul Clozel. (1997) Mibefradil (Ro 40-5967): the first selective T-type Ca2+ channel blocker. Expert Opinion on Investigational Drugs 6:5, pages 569-582.
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H. R. WILTSHIRE, B. M. SUTTON, G. HEEPS, A. M. BETTY, D. W. ANGUS, S. R. HARRIS, E. WORTH & H. A. WELKER. (1997) Metabolism of the calcium antagonist, mibefradil (POSICORTM, Ro 40-5967). Part III. Comparative pharmacokinetics of mibefradil and its major metabolites in rat, marmoset, cynomolgus monkey and man. Xenobiotica 27:6, pages 557-571.
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H. R. WILTSHIRE*B. M. SUTTON, G. HEEPS, A. M. BETTY, D. W. ANGUS, M. J. MADIGAN & S. R. SHARP. (1997) Metabolism of the calcium antagonist, mibefradil (POSICOR™, Ro 40-5967). Part II. Metabolism in hepatic microsomes from rat, marmoset, cynomolgus monkey, rabbit and man. Xenobiotica 27:6, pages 539-556.
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J. A. Bell & M. H. Tarbit. (1992) Twenty years on: a review of the current practice of drug metabolism and pharmacokinetic studies in the pharmaceutical industry. Xenobiotica 22:7, pages 735-742.
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Articles from other publishers (10)

Mohamad Jemain Mohamad Ridhwan, Syahrul Imran Abu Bakar, Normala Abd Latip, Nurunajah Ab Ghani & Nor Hadiani Ismail. (2022) A Comprehensive Analysis of Human CYP3A4 Crystal Structures as a Potential Tool for Molecular Docking-Based Site of Metabolism and Enzyme Inhibition Studies. Journal of Computational Biophysics and Chemistry 21:03, pages 259-285.
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Wenchao Sun, Khoa Dinh Nguyen, William L. Fitch, Samuel D. Banister, Hongxiang Tang, Xiaolan Zhang, Lewis Yu, Edgar G. Engleman & Jayakumar Rajadas. (2018) In vitro and in vivo metabolite identification of a novel benzimidazole compound ZLN005 by liquid chromatography/tandem mass spectrometry . Rapid Communications in Mass Spectrometry 32:6, pages 480-488.
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Nobuo Sekiguchi, Motohiro Kato, Maiko Takada, Hiroo Watanabe, Shotaro Takata, Tetsuya Mitsui, Yoshinori Aso & Masaki Ishigai. (2011) Quantitative Prediction of Mechanism-Based Inhibition Caused by Mibefradil in Rats. Drug Metabolism and Disposition 39:7, pages 1255-1262.
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Peter H. Bui, Arnulfo Quesada, Adrian Handforth & Oliver Hankinson. (2008) The Mibefradil Derivative NNC55-0396, a Specific T-Type Calcium Channel Antagonist, Exhibits Less CYP3A4 Inhibition than Mibefradil. Drug Metabolism and Disposition 36:7, pages 1291-1299.
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Ming Li, J. Bondo Hansen, Luping Huang, Brian M. Keyser & James T. Taylor. (2006) Towards Selective Antagonists of T-Type Calcium Channels: Design, Characterization and Potential Applications of NNC 55-0396. Cardiovascular Drug Reviews 23:2, pages 173-196.
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Maria G. Beconi, Ann Mao, David Q. Liu, Christopher Kochansky, Tony Pereira, Conrad Raab, Paul Pearson & Shuet-Hing Lee Chiu. (2003) METABOLISM AND PHARMACOKINETICS OF A DIPEPTIDYL PEPTIDASE IV INHIBITOR IN RATS, DOGS, AND MONKEYS WITH SELECTIVE CARBAMOYL GLUCURONIDATION OF THE PRIMARY AMINE IN DOGS. Drug Metabolism and Disposition 31:10, pages 1269-1277.
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David Q. Liu & Tony Pereira. (2002) Interference of a carbamoyl glucuronide metabolite in quantitative liquid chromatography/tandem mass spectrometry. Rapid Communications in Mass Spectrometry 16:2, pages 142-146.
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David Q. Liu, Cornelis E.C.A. Hop, Mar�a G. Beconi, Ann Mao & Shuet-Hing Lee Chiu. (2001) Use of on-line hydrogen/deuterium exchange to facilitate metabolite identification. Rapid Communications in Mass Spectrometry 15:19, pages 1832-1839.
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Jean-Paul Clozel, Eric A. Ertel & Sylvie I. Ertel. (1997) Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. Journal of Hypertension 15, pages S17-S26.
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A. Skerjanec & Y.K. Tam. (1995) High-performance liquid chromatographic analysis of mibefradil in dog plasma and urine. Journal of Chromatography B: Biomedical Sciences and Applications 669:2, pages 377-382.
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