Title : The role of P-glycoprotein in the bioactivation of raloxifene.

Pub. Date : 2006 Dec

PMID : 16959878






5 Functional Relationships(s)
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1 The role of P-glycoprotein in the bioactivation of raloxifene. Raloxifene Hydrochloride ATP binding cassette subfamily B member 1 Homo sapiens
2 The aim of this work was to examine the role of P-glycoprotein (Pgp) in the bioactivation of a Pgp substrate, raloxifene, and a non-Pgp substrate, naphthalene. Raloxifene Hydrochloride ATP binding cassette subfamily B member 1 Homo sapiens
3 The aim of this work was to examine the role of P-glycoprotein (Pgp) in the bioactivation of a Pgp substrate, raloxifene, and a non-Pgp substrate, naphthalene. Raloxifene Hydrochloride ATP binding cassette subfamily B member 1 Homo sapiens
4 In addition, the measure of raloxifene-glutathione adducts in the cryopreserved hepatocytes showed that the formation of the adducts increased in the presence of verapamil, which supports the idea that blocking Pgp in the liver increases metabolism and, therefore, the bioactivation of raloxifene. Raloxifene Hydrochloride ATP binding cassette subfamily B member 1 Homo sapiens
5 In addition, the measure of raloxifene-glutathione adducts in the cryopreserved hepatocytes showed that the formation of the adducts increased in the presence of verapamil, which supports the idea that blocking Pgp in the liver increases metabolism and, therefore, the bioactivation of raloxifene. Raloxifene Hydrochloride ATP binding cassette subfamily B member 1 Homo sapiens