Title : S-(+)-Pentedrone and R-(+)-methylone as the most oxidative and cytotoxic enantiomers to dopaminergic SH-SY5Y cells: Role of MRP1 and P-gp in cathinones enantioselectivity.

Pub. Date : 2021 Apr 1

PMID : 33609514






4 Functional Relationships(s)
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1 It was also observed an enantioselectivity in the binding to P-glycoprotein (P-gp), another efflux protein, being the R-(-)-pentedrone and S-(-)-methylone the most transported enantiomeric compounds. methylone ATP binding cassette subfamily B member 1 Homo sapiens
2 It was also observed an enantioselectivity in the binding to P-glycoprotein (P-gp), another efflux protein, being the R-(-)-pentedrone and S-(-)-methylone the most transported enantiomeric compounds. methylone ATP binding cassette subfamily B member 1 Homo sapiens
3 These results were confirmed, in silico, by docking studies, revealing that R-(-)-pentedrone is the enantiomer with highest affinity to MRP1 and S-(-)-methylone and R-(-)-pentedrone are the enantiomers with highest affinity to P-gp. methylone ATP binding cassette subfamily B member 1 Homo sapiens
4 In conclusion, our data demonstrated that pentedrone and methylone present enantioselectivity in their cytotoxicity, which seems to involve, different oxidative reactivity as well as different affinity to the P-gp and MRP1 that together with GSH, play a protective role. methylone ATP binding cassette subfamily B member 1 Homo sapiens