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. Author manuscript; available in PMC: 2019 Sep 12.
Published in final edited form as: J Neurochem. 2008 Jul 1;106(1):147–157. doi: 10.1111/j.1471-4159.2008.05361.x

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
a

All values are in nM.