Table 1.
Drug |
Ki (nM)a |
||
---|---|---|---|
μ-OR | δ-OR | κ-OR | |
IBNTxA | 2.50 ± 0.82 | 0.58 ± 0.16 | 0.23 ± 0.16 |
IBNalA | 0.70 ± 0.18 | 2.55 ± 0.74 | 0.08 ± 0.006 |
KD (nM)b
|
|||
---|---|---|---|
μ-OR | δ-OR | κ-OR | |
IBNTxA | 0.11 ± 0.02 | 0.24 ± 0.005 | 0.027 ± 0.0001 |
IBNalA | 0.22 ± 0.03 | 2.5 ± 0.22 | 0.05 ± 0.22 |
Table adapted from ref. 52.
Competition studies of 125I -radiolabelled compounds against 3H-opioids performed with 3H-DAMGO (μ-OR), 3H-DPDPE (δ-OR), and 3H-U69,593 (κ-OR) at 1 nM concentration in stably transfected CHO Cell lines. Ki values are reported as mean ± SEM; for further details refer to ref 52.
Saturation studies of 125I-labelled compounds in stably transfected CHO cell lines. Kd values are reported as mean ± SEM; for further details refer to ref. 52. Abbreviation: DAMGO, D-Ala-N-MePhe-Glyol-enkephalin; DPDPE, D-Penicillamine-2-D-Penicillamine-5-enkephalin; U69,593, N-methyl-2-phenyl-N-[(5R,7S,8S)-7-pyrrolidin-1-yl-1-oxaspiro[4.5]decan-8-yl]-acetamide.