ArticleBritish journal of pharmacology2006
Modulation of P-glycoprotein activity by cannabinoid molecules in HK-2 renal cells.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 36 citations in OpenAlex.
- Study Models of Drug-Drug Interactions Involving P-Glycoprotein: The Potential Benefit of P-Glycoprotein Modulation at the Kidney and Intestinal Levels.Molecules (Basel, Switzerland) · 2023Review
- The Impact of P-Glycoprotein on Opioid Analgesics: What's the Real Meaning in Pain Management and Palliative Care?International journal of molecular sciences · 2022Review
- Phytochemicals: Potential Lead Molecules for MDR Reversal.Frontiers in pharmacology · 2020Review
- Intestinal P-glycoprotein exports endocannabinoids to prevent inflammation and maintain homeostasis.The Journal of clinical investigation · 2018Article
- Cellular Models and In Vitro Assays for the Screening of modulators of P-gp, MRP1 and BCRP.Molecules (Basel, Switzerland) · 2017Review
- Article
- Enhanced brain disposition and effects of Δ9-tetrahydrocannabinol in P-glycoprotein and breast cancer resistance protein knockout mice.PloS one · 2012Article
- The complications of promiscuity: endocannabinoid action and metabolism.British journal of pharmacology · 2007Review
- The multidrug transporter ABCG2 (BCRP) is inhibited by plant-derived cannabinoids.British journal of pharmacology · 2007Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Endogenous and synthetic cannabinoid molecules have been investigated as possible MDR-1/P-glycoprotein (P-gp) modulators in HK-2-immortalized renal cells, using calcein acetoxymethylester (calcein-AM) as a P-gp substrate. 2. Among the endocannabinoid molecules tested, anandamide (AEA), but not 2-arachidonoyl-glycerol (2-AG) or palmitoyl-ethanolamide (PEA), increased the intracellular fluorescence emitted by calcein, a metabolic derivative of the P-gp substrate calcein-AM, indicative of a reduction in transport capacity. 3. All the three synthetic cannabimimetics tested, that is, R-(+)-methanandamide (R(+)-MET), AM 251 and CP55,940 significantly increased calcein accumulation in the cytosol. 4. RT-PCR demonstrated that HK-2 cells do not express CB1 or CB2 cannabinoid receptors. 5. R(+)-MET, AM251 and CP55,940 were also evaluated as modulators of P-gp expression, by Western blot analysis. Only AM251 weakly enhanced the protein levels (by 1.2-fold) after a 4-day-long incubation with the noncytotoxic drug concentration 2 microM. 6. The present data provide the first evidence that the endocannabinoid AEA and different synthetic cannabinoids may inhibit the P-gp activity in vitro via a cannabinoid receptor-independent mechanism.
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