Skip to main content
. Author manuscript; available in PMC: 2011 Apr 8.
Published in final edited form as: J Med Chem. 2010 Apr 8;53(7):2875–2881. doi: 10.1021/jm9019068

Table 1.

In Vitro Opioid Activity Profiles of Fentanyl Analoguesa

GPI
MVD
Receptor binding
Ki ratio
Cpd IC50 (nM) IC50 (nM) Kiμ (nM) Kiδ (nM) Kiκ (nM) μ/δ/κ
1 22.4 ± 3.7 114 ± 9 0.448 ± 0.079 43.5 ± 4.1 0.536 ± 0.043 1/97/1.2
8a 521 ± 67 5820 ± 1040 300 ± 8 4110 ± 80 238 ± 41 1/14/0.8
8b 590 ± 85 4750 ± 790 224 ± 13 7800 ± 280 162 ± 8 1/35/0.7
10 647 ± 77 610 ± 78 96.0 ± 5.9 6820 ± 670 1850 ± 160 1/71/19
Fentanyl 3.45 ± 0.45b 9.45 ± 4.05b 5.9 ± 1.4c 568 ± 159c 298 ± 40c 1/96/51
LENK 246 ± 39 11.4 ± 1.1 9.43 ± 2.07 2.53 ± 0.35 4570 ± 550 1/0.3/485
a

Values represent means of 3–6 determinations ± SEM.

b

ref.14.

c

ref.15