INHIBITORY EFFECT OF CLEMASTINE ON P-GLYCOPROTEIN EXPRESSION AND FUNCTION: AN IN VITRO AND IN SITU STUDY

Q: How can I download an article?

To download an article from SID, first log in to the site, search for the article title, and click on the 'Download Article' option.

Q: How can I download an ISI article?

To download an ISI article on SID, enter the keyword or article title in the search bar, view the relevant results, click on the desired article, and select the 'Download Article' option.

Q: How can I access the SID database?

To access the SID database, visit SID.ir, create an account, and log in to access scientific resources.

Q: Is downloading articles from SID free?

Some articles on SID are available for free, while others require payment. Details are specified on the article's page.

MESGARI ABBASI MEHRAN; VALIZADEH HADI; HAMISHEHKAR HAMED; MOHAMMADNEJAD LEILA; ZAKERI MILANI PARVIN

مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

Journal Paper

Paper Information

Journal: Iranian Journal of Basic Medical Sciences Year:2016 | Volume:19 | Issue:4 Page(s): 423-429

Download Full-Text

View:

242

Download:

180

Cites:

Information Journal Paper

Title

INHIBITORY EFFECT OF CLEMASTINE ON P-GLYCOPROTEIN EXPRESSION AND FUNCTION: AN IN VITRO AND IN SITU STUDY

Author(s)

Keywords

CLEMASTINE

DIGOXIN

INTESTINAL ABSORPTION

P-GLYCOPROTEIN

Abstract

Objective (s): Transporters have an important role in pharmacokinetics of drugs. Inhibition or induction of drug transporters activity can affect drug absorption, safety, and efficacy. P-GLYCOPROTEIN (P-gp) is the most important membrane transporter that is responsible for active efflux of drugs. It is important to understand which drugs are substrates, inhibitors, or inducers of P-gp to minimize or avoid unwanted interactions. The aim of this study was to investigate the effects of CLEMASTINE on the expression and function of P-gp.Materials and Methods: The effect of CLEMASTINE on P-gp function and expression was evaluated in vitro byrhodamine-123 (Rho123) efflux assay in Caco-2 cells and Western blot analysis. Rat in situ single pass intestinal permeability model was used to investigate the CLEMASTINE effect on DIGOXIN Peff, as a known P-gp substrate. DIGOXIN levels in intestinal perfusates were assayed by high performance liquid chromatography (HPLC) method.Results: The Caco-2 intracellular accumulation of Rho123 in CLEMASTINE and verapamil treated cells was 90.8 ± 9.8 and 420.6±25.4 pg/mg protein, respectively which was significantly higher than that in control cells (50.2±6.0; P<0.05). Immunoblotting results indicated that CLEMASTINE decreased expression of P-gp in Caco-2 cells in vitro. More over effective intestinal permeability (Peff) of DIGOXIN in the presence of CLEMASTINE, was significantly increased compare to control group.Conclusion: Findings of our study suggested dose dependent P-gp inhibition activity for CLEMASTINE in vitro and in situ. Therefore co-administration of CLEMASTINE with P-gp substrates may result in unwanted interactions and side effects.

Cites

No record.

References

No record.

Cite

APA: Copy

MESGARI ABBASI, MEHRAN, VALIZADEH, HADI, HAMISHEHKAR, HAMED, MOHAMMADNEJAD, LEILA, & ZAKERI MILANI, PARVIN. (2016). INHIBITORY EFFECT OF CLEMASTINE ON P-GLYCOPROTEIN EXPRESSION AND FUNCTION: AN IN VITRO AND IN SITU STUDY. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 19(4), 423-429. SID. https://sid.ir/paper/678474/en

Vancouver: Copy

MESGARI ABBASI MEHRAN, VALIZADEH HADI, HAMISHEHKAR HAMED, MOHAMMADNEJAD LEILA, ZAKERI MILANI PARVIN. INHIBITORY EFFECT OF CLEMASTINE ON P-GLYCOPROTEIN EXPRESSION AND FUNCTION: AN IN VITRO AND IN SITU STUDY. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2016;19(4):423-429. Available from: https://sid.ir/paper/678474/en

IEEE: Copy

MEHRAN MESGARI ABBASI, HADI VALIZADEH, HAMED HAMISHEHKAR, LEILA MOHAMMADNEJAD, and PARVIN ZAKERI MILANI, “INHIBITORY EFFECT OF CLEMASTINE ON P-GLYCOPROTEIN EXPRESSION AND FUNCTION: AN IN VITRO AND IN SITU STUDY,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 19, no. 4, pp. 423–429, 2016, [Online]. Available: https://sid.ir/paper/678474/en

Related Journal Papers

No record.

Related Seminar Papers

No record.

Related Plans

No record.

Recommended Workshops