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Xenobiotica
the fate of foreign compounds in biological systems
Volume 27, 1997 - Issue 6
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Research Article

Metabolism of the calcium antagonist, mibefradil (POSICOR™, Ro 40-5967). Part II. Metabolism in hepatic microsomes from rat, marmoset, cynomolgus monkey, rabbit and man

H. R. WILTSHIRE* Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
,
B. M. SUTTON Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
,
G. HEEPS Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
,
A. M. BETTY Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
,
D. W. ANGUS Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
,
M. J. MADIGAN Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
&
S. R. SHARP Pharmacokinetics and Metabolism Department, Roche Products Ltd, 40 Broadwater Road, Welwyn Garden City AL7 3AY, UK
 show all
Pages 539-556 | Published online: 22 Sep 2008

References

  • BERNINK, J. J. L. M., PRAGER, G., SCHELLING, A. and KOBRIN, I., 1996, Antihypertensive properties of the novel calcium antagonist mibefradil (Ro 40–5967). A new generation of calcium antagonists? Hypertension, 27, 426–432.
  • CLOZEL, J.-P., BANKEN, L. and OSTERRIEDER, W., 1989, Effects of Ro 40-5967, a novel calcium antagonist, on myocardial function during ischemia induced by lowering coronary perfusion pressure in dogs: comparison with verapamil. Journal of Cardiovascular Pharmacology, 14, 713–721.
  • CLOZEL, J.-P., 0 STERR1EDER, W., KLEINBLOESSEM C. H., WELKER, H. A., SCHLAPPI, B., TUDOR, R., HEFTI, H., SCHMITT, R. and EGGERS, H., 1991, Ro 40–5967: a new non-dihydropyridine calcium antagonist. Cardiovascular Drug Reviews, 9, 4–17.
  • MISHRA, S. K. and HERMAMEYER, K., 1994, Selective inhibition of T-type Ca2+ channels by Ro 40-5967, Circulation Research, 75, 144–148.
  • OMURA, T. and SATO, R., 1964, The carbon monoxide binding pigment of liver microsomes. journal of Biological Chemistry, 239, 2370–2378.
  • OPERIL, S. and CALHOUN, D. A., 1991, The calcium antagonist in the 1990s: an overview. American Journal of Hypertension, 4, 396S–405S.
  • OSTERR1EDER, W. and HoLcK, M., 1989, In vitro pharmacologic profile of Ro 40-5967, a novel Ca2+ channel blocker with potent vasodilator but weak inotropic action. Journal of Cardiovascular Pharmacology, 13, 754–759.
  • PORTEGlES, M. C. M., SCHMITT, R., KRAALI, C. J., BRAAT, S. H. J. G., GUSSNER, A., HAGERMEIJER, F., POZENEL, H., PRAGER, G., VlERSMA, J. W., VAN DER WALL, E. E., KLEINBLOESSEM, CH. and LlE, K. E., 1991, Lack of negative inotropic effects of the new calcium antagonist Ro 40–5967 in patients with chronic stable angina pectoris . Journal of Cardiovascular Pharmacology, 18, 746–751.
  • RUTLEDGE, A. and TRIGGLE, D. J., 1995, The binding interactions of Ro 40-5967 at the L-type Ca2+ channel in cardiac tissue. European Journal of Pharmacology, 290, 155–158.
  • TRIGGLE, D. J., 1991, Sites, mechanism of action and differentiation of calcium channel antagonists. America Journal of Hypertension, 4, 422S–429S.
  • WELKER, H. A., EGGERS, H., KLEINBLOESSEM, CH., ERB, K., BREITHAUPT, K., BUTZER, R. and BELZ, G. G., 1989, Ro 40–5967: pharmacokinetics of a new calcium antagonist. European Journal of Clinical Pharmacology, 36 (suppl.), A304.
  • WILTSHIRE, H. R., HARRIS, S. R., PRIOR, K. J., KOZLOWSKI, U. M. and WORTH, E., 1992, Metabolism of calcium antagonist Ro 40-5967: a case history of the use of diode-array UV spectroscopy and thermospray-mass spectrometry in the elucidation of a complex metabolic pathway. Xenobiotica, 22, 837–857.
  • WILTSHIRE, H. R., SUTTON, B. M., HEEPS, G., BETTY, A. M., ANGUS, D. W., HARRIS, S. R. and WORTH, E., 1997, Metabolism of the calcium antagonist, mibefradil (POSICOR, Ro 40-5967). Part III. Comparative pharmacokinetics of mibefradil and its major metabolites in rat, marmoset, cynomolgus monkey and man. Xenobiotica, 27, 557–572.
  • WOOD, A., 1989, Calcium antagonists: pharmacological differences and similarities. Circulation, 80 (suppl. IV), IV.84–88.

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