Jean-Michel Scherrmann

2 papers in the library · 136 citations · publishing 2009-2010

Papers

Interaction of drugs of abuse and maintenance treatments with human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2).

The international journal of neuropsychopharmacology August 1, 2010 Nicolas Tournier, Lucie Chevillard, Bruno Megarbane et al. 122 citations

Several drugs used in addiction treatment and substances of abuse inhibit the efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) in vitro, which could alter their distribution in the body, including across the blood-brain barrier. Norbuprenorphine, buprenorphine, methadone, ibogaine, and THC inhibited P-gp in a concentration-dependent manner, with norbuprenorphine being the strongest. Buprenorphine, norbuprenorphine, ibogaine, and THC inhibited BCRP. Cocaine, amphetamine, nicotine, morphine, and others did not inhibit either transporter. Norbuprenorphine and methadone were transported by P-gp, but no tested compounds were transported by BCRP. The clinical relevance of norbuprenorphine's interaction with P-gp remains unclear.

DOI: 10.1017/S1461145709990848 Full text Ibogaine THC Drug transport Drug movement +22

Ibogaine labeling with 99mTc-tricarbonyl: synthesis and transport at the mouse blood-brain barrier.

Journal of pharmaceutical sciences December 1, 2009 Nicolas Tournier, Pascal André, Sandy Blondeel et al. 14 citations

Radiolabeling the neuroactive compound ibogaine with technetium-99m tricarbonyl produced a tracer that entered the mouse brain poorly, at a rate similar to other tracers known to have low brain uptake. The brain entry rate was about 70 times lower than that of a standard clinical brain-imaging agent. Neither the labeled ibogaine nor the tricarbonyl core alone were substrates for the main efflux transporters at the blood-brain barrier. Instead, the limited brain penetration was attributed to the compound's lipophilicity and its interaction with the membrane's positive dipole potential, as lowering that potential with phloretin increased transport roughly threefold. The findings indicate that ibogaine directly labeled with this radionuclide is unsuitable for central nervous system imaging.

DOI: 10.1002/jps.21771 Full text Brain imaging Neuroimaging Molecular imaging Imaging agents +23