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Paquay JB, Bolscher MT, Voss HP, et al. Difference in the inhibition of nitric oxide synthase and cytochrome P-450 by some H(2)-antagonists. Toxicol In Vitro. 1997;11(6):775-8doi: 10.1016/s0887-2333(97)00035-0.
Paquay, J. B., Bolscher, M. T., Voss, H. P., Timmerman, H., & Bast, A. (1997). Difference in the inhibition of nitric oxide synthase and cytochrome P-450 by some H(2)-antagonists. Toxicology in vitro : an international journal published in association with BIBRA, 11(6), 775-8. https://doi.org/10.1016/s0887-2333(97)00035-0
Paquay, J B, et al. "Difference in the inhibition of nitric oxide synthase and cytochrome P-450 by some H(2)-antagonists." Toxicology in vitro : an international journal published in association with BIBRA vol. 11,6 (1997): 775-8. doi: https://doi.org/10.1016/s0887-2333(97)00035-0
Paquay JB, Bolscher MT, Voss HP, Timmerman H, Bast A. Difference in the inhibition of nitric oxide synthase and cytochrome P-450 by some H(2)-antagonists. Toxicol In Vitro. 1997 Dec;11(6):775-8. doi: 10.1016/s0887-2333(97)00035-0. PMID: 20654383.
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Toxicol In Vitro. 1997 Dec;11(6):775-8. doi: 10.1016/s0887-2333(97)00035-0.

Difference in the inhibition of nitric oxide synthase and cytochrome P-450 by some H(2)-antagonists.

Toxicology in vitro : an international journal published in association with BIBRA

J B Paquay, M T Bolscher, H P Voss, H Timmerman, A Bast

Affiliations

  1. Leiden/Amsterdam Center for Drug Research, Division of Molecular Pharmacology, Department of Pharmacochemistry, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands.

PMID: 20654383 DOI: 10.1016/s0887-2333(97)00035-0

Abstract

The enzyme nitric oxide synthase (NOS) is reported to have some similarities to the family of cytochrome P-450 enzymes. In this study the histamine H(2)-antagonists 2-methyl-4(4-isopropylaminomethyleneiminophenyl) imidazole (DA 5047), 2-guanidino-4(3-methylaminomethyleneiminophenyl)thiazole (DA 4643), tiotidine and cimetidine, which all display cytochrome P-450 inhibition were tested in a rat brain constitutive NOS (cNOS) assay. It was found that all four compounds inhibit rat brain cNOS in a competitive way. This was compared with the inhibition of cytochrome P-450 by these compounds reported previously by Rekka et al. (Rekka et al., 1989). The pIC(50) for cNOS inhibition correlated negatively with the pIC(50) found for P-450 inhibition. Apparently, the H(2)-antagonists interact differently to NOS compared with cytochrome P-450, indicating that there is a functional difference in the molecular mechanism of both enzymes in contrast to what has been suggested.

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