Selected pharmacological characteristics of fluoroprobes 6, 7, and 8a.
Probe | Alog P | K i [nM] | cAMP EC50 [nM] (% efficacy) | ||||
---|---|---|---|---|---|---|---|
hCB2R | hCB1R | mCB2R | mCB1R | hCB2R | hCB1R | ||
(S)-6-NBD | 6.3 | 9.1 | 617 | 33 | 691 | 2.2 (72) | >10 000 |
(R)-6-NBD | 6.3 | 159 | 4925 | 622 | n.d. | 17 (84) | >10 000 |
(S)-7-AF488 | 5.3 | 44 | 321 | 28 | >10 000 | 1.3 (100) | 86 (109) |
(S)-8-SiR | 10.6 | 62 | 114 | 117 | 1892 | 67 (96) | >10 000 |
See ESI, S10 for detailed description of the assay protocols.