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. Author manuscript; available in PMC: 2012 Jul 22.
Published in final edited form as: Int J Pharm. 2009 Apr 5;375(1-2):48–54. doi: 10.1016/j.ijpharm.2009.03.037

Table 1.

Fold stimulation of basal P-gp-ATPase activity by a series of morphine and meperi-dine analogs.

Compound n Fold stimulation
Morphine analogs
 Non-treated (control) 4 1.00 ± 0.04
 Morphinea 4 1.54 ± 0.08b
N-Benzylcodeinec 4 1.01 ± 0.14
 6-Desoxymorphined 4 1.01 ± 0.11
 Oxymorphonee 4 1.12 ± 0.12
 Thevinonef 4 1.28 ± 0.05b
 Methyl thevinolf 4 1.28 ± 0.04b
 Etorphine-3-methyl etherf 4 1.29 ± 0.10
 6-Desoxycodeined 4 1.31 ± 0.15
 Etorphinef 4 1.34 ± 0.08b
 Codeinea 4 1.36 ± 0.07b
 Naloxonea 4 1.25 ± 0.11
 Naltrexonea 4 1.13 ± 0.05
Meperidine analogsg
 Non-treated (control) 4 1.00 ± 0.03
 Meperidine 3 1.51 ± 0.29
N-Phenylbutyl normeperidine 3 1.10 ± 0.23
N-Propyl normeperidine 3 1.81 ± 0.23b
N-2-Methylpropyl normeperidine 3 1.88 ± 0.22b
N-Methylallyl normeperidine 3 2.00 ± 0.41b
N-Butyl normeperidine 3 2.06 ± 0.19b
N-Phenylpropyl normeperidine 3 2.38 ± 0.12b
N-Crotyl normeperidine 3 2.80 ± 0.13b
N-Benzyl normeperidine 3 2.94 ± 0.07b
N-Allyl normeperidine 3 2.95 ± 0.29b
N-Phenylethyl normeperidine 3 3.66 ± 0.15b

Results are represented as mean ± S.E.M. The positive controls, verapamil and methadone stimulated the P-gp basal activity by 5.41 ± 1.52 and 2.45 ± 0.27-folds (Hassan et al., 2009), respectively.

a

Indicates compounds purchased or supplied as gifts from Mallinckrodt, Inc. (St. Louis, MO).

b

Indicates significant differences (p < 0.05) from corresponding control as determined by Student’s t-test.

c

Indicates a compound synthesized according to Koczka and Bernath (1958).

d

Indicates compounds synthesized according to Rapoport and Bonner (1951).

e

Indicates a compound synthesized according to Iijima et al. (1978).

f

Indicates compounds synthesized according to Bentley et al. (1967).

g

Meperidine analogs data were previously reported as change in luminescence (Mercer et al., 2007) and represented in the table for comparison with the morphine analogs.