Pregnane X receptor and constitutive androstane receptor modulate differently CYP3A-mediated metabolism in early- and late-stage cholestasis

doi:10.3748/wjg.v23.i42.7519

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World Journal of Gastroenterology

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1007-9327

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Baishideng Publishing Group Inc, 7041 Koll Center Parkway, Suite 160, Pleasanton, CA 94566, USA

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World J Gastroenterol. Nov 14, 2017; 23(42): 7519-7530
Published online Nov 14, 2017. doi: 10.3748/wjg.v23.i42.7519

Table 3 Kinetic parameters for 4- and 1’-hydroxylation activities of microsomal preparations obtained from sham-operated and cholestatic rats

	4-OH MDZ		1’-OH MDZ
	Vmax (pmol/mg/min)	Km (μmol/L)	Vmax (pmol/mg/min)	Km (μmol/L)
Sham-operated rats	1009.9 ± 269.4	3.4 ± 1.1	946.7 ± 292.2	2.5 ± 0.9
Mildly cholestatic rats	1116.0 ± 333.7	3.5 ± 1.4	1017.0 ± 317.4	2.8 ± 1.6
Severely cholestatic rats	218.4 ± 88.1^c^f	6.1 ± 4.7	200.1 ± 68.7^c^f	4.3 ± 2.6

The results are reported as mean ± SD of 8 rats per group.

^cP < 0.001 vs sham-operated rats;

^fP < 0.001 vs mildly cholestatic rats.

Citation: Gabbia D, Pozza AD, Albertoni L, Lazzari R, Zigiotto G, Carrara M, Baldo V, Baldovin T, Floreani A, Martin SD. Pregnane X receptor and constitutive androstane receptor modulate differently CYP3A-mediated metabolism in early- and late-stage cholestasis. World J Gastroenterol 2017; 23(42): 7519-7530
URL: https://www.wjgnet.com/1007-9327/full/v23/i42/7519.htm
DOI: https://dx.doi.org/10.3748/wjg.v23.i42.7519