Table 2:
Affinities of H1 antagonists compared to cocaine at H1 histamine receptors, monoamine transporters and potency as inhibitors of DA uptakea.
Compound | H1 Ki Value (± SEM) | DAT Ki Value (± SEM) | SERT Ki Value (± SEM) | NET Ki Value (± SEM) | DA Uptake Inhibition IC50 Value (± SEM) |
---|---|---|---|---|---|
Triprolidine | 27.7 ± 2.06 | 6010 ± 475 | 3340 ± 134 | 12800 ± 487 | 19000 ± 2520 |
(+)-Chlorpheniramine | 37.9 ± 1.08 | 203 ± 20.0 | 25.4 ± 2.03 | 6140 ± 845 | 669 ± 54.9 |
Diphenhydramine | 96.0 ± 7.43 | 851 ± 72.2 | 9050 ± 699 | 2070 ± 159 | 2080 ± 115 |
(−)-Chlorpheniramine | 506 ± 69 | 383 ± 15.5 | 355 ± 47.8 | 5390 ± 782 | 1420 ± 144 |
Cocaine | 1040 ± 43.0 | 71.8 ± 4.56 | 293 ± 30 | 2120 ± 314 | 293 ± 30 |
All values are in nM.