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Drug Design, Development and Therapy Volume 10, 2016 - Issue
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Original Research

Role of cytochrome P450 2D6 genetic polymorphism in carvedilol hydroxylation in vitro

Zhe Wang1 Department of Pharmacy, The Second Affiliated Hospital & Yuying Children’s Hospital of Wenzhou Medical University, Wenzhou, People’s Republic of China
,
Li Wang2 Department of Pharmacology, School of Pharmacy, Wenzhou Medical University, Wenzhou, People’s Republic of China;3 Department of Pharmacy, Women’s Hospital, School of Medicine, Zhejiang University, Hangzhou, People’s Republic of China
,
Ren-ai Xu4 Department of Pharmacy, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, People’s Republic of China
,
Yun-yun Zhan2 Department of Pharmacology, School of Pharmacy, Wenzhou Medical University, Wenzhou, People’s Republic of China
,
Cheng-ke Huang1 Department of Pharmacy, The Second Affiliated Hospital & Yuying Children’s Hospital of Wenzhou Medical University, Wenzhou, People’s Republic of China
,
Da-peng Dai5 The Key Laboratory of Geriatrics, Beijing Hospital & Beijing Institute of Geriatrics, Ministry of Health, Beijing, People’s Republic of China
,
Jian-ping Cai5 The Key Laboratory of Geriatrics, Beijing Hospital & Beijing Institute of Geriatrics, Ministry of Health, Beijing, People’s Republic of ChinaCorrespondence[email protected]
&
Guo-xin Hu2 Department of Pharmacology, School of Pharmacy, Wenzhou Medical University, Wenzhou, People’s Republic of ChinaCorrespondence[email protected]
 show all
Pages 1909-1916 | Published online: 08 Jun 2016

Figures & data

Figure 1 Structure of the analytes and metabolic pathway of carvedilol.

Abbreviations: CYP2D6, cytochrome P450 2D6; CYP2C9, cytochrome P450 2C9.
Figure 1 Structure of the analytes and metabolic pathway of carvedilol.

Table 1 Kinetic parameters for carvedilol 4′-hydroxylation activities of recombinant wild-type and mutant CYP2D6 proteins

Table 2 Kinetic parameters for carvedilol 5′-hydroxylation activities of recombinant wild-type and mutant CYP2D6 proteins

Figure 2 Michaelis–Menten curves of the carvedilol 4′-hydroxylation activities of the recombinant wild-type CYP2D6 protein and the 24 variants toward carvedilol.

Note: Each point represents the mean ± SD of three separate experiments.
Abbreviations: CYP2D6, cytochrome P450 2D6; min, minute.
Figure 2 Michaelis–Menten curves of the carvedilol 4′-hydroxylation activities of the recombinant wild-type CYP2D6 protein and the 24 variants toward carvedilol.

Figure 3 Michaelis–Menten curves of the carvedilol 5′-hydroxylation activities of the recombinant wild-type CYP2D6 protein and the 24 variants toward carvedilol.

Note: Each point represents the mean ± SD of three separate experiments.
Abbreviations: CYP2D6, cytochrome P450 2D6; min, minute.
Figure 3 Michaelis–Menten curves of the carvedilol 5′-hydroxylation activities of the recombinant wild-type CYP2D6 protein and the 24 variants toward carvedilol.

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