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. Author manuscript; available in PMC: 2009 Dec 25.
Published in final edited form as: J Med Chem. 2008 Dec 25;51(24):7866–7881. doi: 10.1021/jm800913d

Table 3.

Functional data ([35S]GTP-γ-S)a for the N-phenethyl substituted para- (16) and ortho-b isomers (24)

graphic file with name nihms78004f15.jpg
16: R1 = H, R2 = OH
24: R1 = OH, R2 = H
Cmpd # μ-Antagonism Ke (nM)b δ-Antagonism Ke (μM)c κ-Antagonism Ke (nM)c
16 260 ± 79 17 ± 4.2 19 ± 5.2
24 77 ± 13 8 ± 1.5 21 ± 3.4
Naloxone 2.3 ± 0.3 - -
Naltrindole - 0.18 ± 0.01 -
norBNI - - 0.11 ± 0.02
a

[35S]-GTP-γ-S binding was conducted as previously described.19, 20

b

For μ-receptors, Ke values were calculated according to the equation: [test drug]/(EC50-2/EC50-1 − 1), where EC50-2 is the EC50 value of DAMGO in the presence of a fixed concentration of the test drug and EC50-1 is the value in the absence of the test drug.

c

For δ and κ receptors, Ke values were determined as described in the section “Data analysis and statistics” in Hiebel et al.19 Each parameter value is ± SD.