Table 1.
Effects of Selected Organic Compounds, Psychoactive Drugs, and Their Metabolites (A) and Cocaine Metabolites (B) on [3H]-Cocaine Uptake in hCMEC/D3 Cellsa
| Compound | Concentration, mM | Relative uptake, % |
|---|---|---|
| A | ||
| Carnitine | 5 | 96.1±15.0 |
| Choline | 5 | 102.0±14.2 |
| TEA | 5 | 120.6±9.8 |
| Nicotine | 0.05 | 73.8±2.6* |
| MDMA | 0.05 | 29.7±0.7*** |
| MDPV | 0.05 | 18.1±0.4*** |
| Clonidine | 0.05 | 17.3±1.3*** |
| Diphenhydramine | 0.05 | 8.3±0.4*** |
| Verapamil | 0.05 | 3.7±0.2*** |
| Imipramine | 0.05 | 1.6±0.4*** |
| Oxycodone | 0.05 | 68.7±4.4*** |
| Codeine | 0.05 | 63.4±5.0** |
| Morphine | 0.05 | 62.9±14.7** |
| Hydrocodone | 0.05 | 49.2±5.8*** |
| Oxymorphone | 0.05 | 36.3±1.1*** |
| Norbuprenorphine | 0.05 | 31.7±6.3** |
| 6-Acetylcodeine | 0.05 | 31.3±1.7*** |
| Naloxone | 0.05 | 28.3±0.9*** |
| Heroin | 0.05 | 20.6±0.6*** |
| Tramadol | 0.05 | 19.3±2.0*** |
| Methadone | 0.05 | 6.1±0.3*** |
| B | ||
| Benzoylecgonine | 0.05 | 104.1±3.0 |
| 0.1 | 94.2±14.9 | |
| 1 | 72.0±11.4* | |
| Ecgonine | 0.05 | 103.9±8.7 |
| 0.1 | 93.2±2.5 | |
| 1 | 75.3±5.0* | |
| Ecgoninemethylester | 0.01 | 62.9±4.0*** |
| 0.05 | 27.7±2.2*** | |
| 0.1 | 18.3±3.4*** | |
| Cocaethylene | 0.01 | 35.4±4.4*** |
| 0.05 | 15.3±0.3*** | |
| 0.1 | 12.0±0.6*** | |
| Norcocaine | 0.01 | 29.5±1.1*** |
| 0.05 | 18.2±0.1*** | |
| 0.1 | 13.5±0.3*** | |
Abbreviations: MDMA, 3,4-methylenedioxyamphetamine; MDPV, 3,4-methylenedioxypyrovalerone; TEA, tetraethylammonium.
aThe inhibition of the transport of [3H]-cocaine (3nM) by the above compounds was evaluated in hCMEC/D3 cells with Krebs-HEPES buffer (pHe 7.40) and an incubation time of 5min. The uptake rate for controls set at 100±10% was 0.105±0.01 µL/min/µg. Data are expressed as means ± SD (performed in triplicate). * P<0.05, ** P<0.01, *** P<0.001 compared with the control group.