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. 2021 Apr 6;22(7):3779. doi: 10.3390/ijms22073779

Table 2.

Competition of [3H]DAMGO binding in Chinese Hamster Ovary (CHO) cells stably expressing mouse, rat and human Oprm1 7TM C-terminal variants.

Ligand
Ki Value (nM) DAMGO Morphine Fentanyl Methadone M6G β-Endorphin Dynorphin A Endomorphin 1 Endomorphin 2 [Met]5Enkephalin-Arg6-Phe7 Refs.
Mouse
mMOR-1 1.8 ± 0.5 5.3 ± 2.0 2.3 ± 1.0 1.4 ± 0.1 5.2 ± 1.8 11 ± 2.9 11 ± 0.5 2.1 ± 0.8 4.2 ± 1.8 4.1 ± 1.0 [73,100]
mMOR-1A 1.0 ± 0.3 3.1 ± 0.5 1.5 ± 0.6 0.7 ± 0.1 5.0 ± 1.5 4.3 ± 1.0 8.2 ± 2.8 3.5 ± 1.3 [73,77]
mMOR-1C 0.93 ± 0.2 2.4 ± 0.6 1.2 ± 0.4 0.5 ± 0.1 4.1 ± 1.2 5.8 ± 0.5 5.6 ± 0.8 1.4 ± 0.4 1.6 ± 0.2 2.1 ± 0.7 [73,100]
mMOR-1D 0.71 ± 0.1 1.5 ± 0.2 3.3 ± 1.5 1.4 ± 0.1 4.8 ± 0.8 1.7 ± 0.4 2.2 ± 0.8 1.8 ± 0.3 2.0 ± 0.3 3.7 ± 1.2 [73,100]
mMOR-1E 1.2 ± 0.5 2.3 ± 0.4 1.2 ± 0.5 0.7 ± 0.3 5.6 ± 0.7 5.0 ± 1.2 8.9 ± 1.1 2.4 ± 0.1 4.4 ± 0.8 4.4 ± 0.9 [73,100]
mMOR-1B1 1.4 ± 0.2 5.3 ± 1.0 10 ± 1.6 6.8 ± 3.2 15 ± 7.1 11 ± 5.6 12 ± 1.5 [75]
mMOR-1B2 1.3 ± 0.1 3.9 ± 0.4 8.4 ± 1.3 4.9 ± 1.7 34 ± 18 5.0 ± 1.8 8.4 ± 1.1 [75]
mMOR-1B3 1.8 ± 0.9 1.5 ± 0.5 3.9 ± 1.3 3.1 ± 1.4 8.7 ± 1.8 3.2 ± 0.6 3.2 ± 0.8 [75]
mMOR-1B5 1.0 ± 0.3 1.4 ± 0.6 5.2 ± 0.1 5.7 ± 1.2 8.9 ± 2.3 4.3 ± 0.8 11 ± 1.8 [75]
mMOR-1F 1.1 ± 0.2 2.9 ± 0.5 1.7 ± 0.5 1.3 ± 0.2 9.6 ± 0.8 6.0 ± 1.6 12 ± 1.0 2.9 ± 0.5 4.1 ± 1.3 3.9 ± 0.8 [73,78]
mMOR-1O 3.3 ± 1.2 2.7 ± 0.6 17 ± 1.0 16 ± 5.3 58 ± 26 [77]
mMOR-1P 0.8 ± 0.3 1.2 ± 0.8 11 ± 3.4 5.9 ± 2.4 103 ± 23 [77]
Rat
rMOR-1 3.3 ± 0.6 5.6 ± 0.8 17 ± 2.2 3.7 ± 0.4 12 ± 3.0 4.1 ± 0.7 8.0 ± 2.0 [74]
rMOR-1A 6.0 ± 0.9 8.0 ± 0.4 26 ± 2.1 11 ± 0.6 23 ± 1.6 6.5 ± 0.3 12 ± 0.6 [74]
rMOR-1C1 4.5 ± 0.9 7.4 ± 0.3 25 ± 2.4 8.8 ± 0.5 13 ± 2.3 3.9 ± 0.1 10 ± 0.6 [74]
rMOR-1D 4.7 ± 1.2 7.4 ± 0.5 21 ± 1.8 8.5 ± 0.6 11 ± 1.7 3.9 ± 0.4 7.5 ± 0.4 [74]
Human
hMOR-1 1.2 ± 0.2 2.2 ± 0.9 10 ± 0.3 15 ± 11.0 87 ± 14 4.2 ± 1.4 15 ± 7.1 [76]
hMOR-1B1 1.2 ± 0.4 2.4 ± 1.1 5.0 ± 0.2 7.8 ± 1.5 19 ± 6.6 3.8 ± 0.8 5.4 ± 0.6 [76]
hMOR-1B2 5.2 ± 1.4 11 ± 3.5 42 ± 7.9 25 ± 5.1 49 ± 22 12 ± 0.1 20 ± 1.3 [76]
hMOR-1B3 1.8 ± 0.5 3.2 ± 0.6 16 ± 1.2 8.2 ± 2.2 14 ± 2.3 4.9 ± 1.5 6.3 ± 1.5 [76]
hMOR-1B4 2.3 ± 0.6 5.5 ± 1.7 23 ± 7.4 16 ± 0.4 71 ± 30 9.9 ± 2.3 23 ± 2.0 [76]
hMOR-1B5 2.1 ± 0.4 3.9 ± 0.9 12 ± 2.6 10 ± 3.4 53 ± 23 4.6 ± 0.3 9.6 ± 3.0 [76]
hMOR-1O 2.2 ± 0.6 2.0 ± 0.7 16 ± 2.6 25 ± 8.5 [79]
hMOR-1X 2.1 ± 0.2 2.7 ± 1.0 17 ± 5.3 187 ± 27 [79]
hMOR-1Y 2.5 ± 0.8 4.3 ± 1.7 8.3 ± 2.2 8.4 ± 1.8 25 ± 13 5.1 ± 1.1 9.4 ± 3.0 [76]

[3H]DAMGO binding was performed with membranes prepared from CHO cells stably expressing indicated splice variants, as described in indicated references.