Table 2.
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.