Bromocriptine Modulates P-Glycoprotein Function
Biochemical and Biophysical Research Communications, ISSN: 0006-291X, Vol: 244, Issue: 2, Page: 481-488
1998
- 40Citations
- 14Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations40
- Citation Indexes40
- 40
- CrossRef17
- Captures14
- Readers14
- 14
Article Description
The multidrug resistance (MDR)-associated P-glycoprotein (P-gp) is a membrane transporter which carries, at the expense of MgATP hydrolysis, many amphiphilic molecules, such as the MDR-related cytotoxic drugs vincristine and vinblastine, and the MDR-reversing agents verapamil and progesterone. We have tested the effects on P-gp function of bromocriptine (BCT), an ergot alkaloid known as a D2 dopaminergic receptor agonist. BCT (at 4 μM) partially reverses the P-gp-mediated vincristine resistance of the Chinese hamster lung fibroblasts DC-3F/ADX, a MDR cell line. P-gp containing membrane vesicles prepared from the DC-3F/ADX cells exhibit, in the absence of any added drug, a basal MgATPase activity due to P-gp. BCT inhibits this basal ATPase activity, with a half-inhibiting concentration of 0.30 ± 0.15 μM. BCT also inhibits the verapamil-induced P-gp ATPase stimulation competitively (K i ≈ 0.2 μM), and the progesterone-induced P-gp ATPase stimulation non-competitively (K i ≈ 0.07-0.10 μM). BCT also non-competitively inhibits the vinblastine-dependent P-gp ATPase activity within the same concentration range. Hydroxylated metabolites of BCT have different effects on P-gp ATPase, only the monohydroxylated being able to modulate both the basal and the drug-stimulated ATPase activities. In conclusion, these effects of BCT on P-gp function can be linked to a specific interaction with P-gp, probably involving inhibition of P-gp-mediated drug transport.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0006291X98982894; http://dx.doi.org/10.1006/bbrc.1998.8289; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=0032539760&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/9514944; https://linkinghub.elsevier.com/retrieve/pii/S0006291X98982894; https://dx.doi.org/10.1006/bbrc.1998.8289
Elsevier BV
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