Table 1.
Competition opioid binding assays with125I-BNtxA in triple-KO and WT mice brain membranes
| Drug |
Ki |
|
| Triple-KO, nM | WT with blockers, nM | |
| Mu | ||
| Fentanyl | 226 ± 40 | 256 ± 10.2 |
| β-Funaltrexamine | 35.6 ± 5.3 | 37.8 ± 10.6 |
| Naloxone | 51.9 ± 1.4 | 53.2 ± 7.13 |
| Naltrexone | 20.5 ± 1.8 | 32.7 ± 4.1 |
| Kappa1 | ||
| 5′-Guanidinonaltrindole (GNTI) | 22.9 ± 3.3 | 29.1 ± 0.02 |
| Norbinaltorphimine (NOR-BNI) | 3.3 ± 1.9 | 4.94 ± 0.99 |
| Delta | ||
| Naltrindole | 26.3 ± 2.3 | 28.09 ± 10.96 |
| Kappa3 | ||
| NalBzoH | 0.59 ± 0.15 | 1.0 ± 0.3 |
| Nalorphine | 3.71 ± 1.45 | 7.5 ± 0.6 |
| Levorphanol | 8.8 ± 2.5 | 5 ± 1.5 |
| Levallorphan | 0.34 ± 0.018 | 0.5 ± 0.15 |
| Ketocyclazocine | 0.04 ± 0.01 | 3.14 ± 1.08 |
| (−)-SKF10,047 | 13.5 ± 1.6 | 22.2 ± 1.9 |
| Mr2034 | 2.67 ± 0.83 | 3.99 ± 1.1 |
| (−)Ethylketocyclazocine | 0.21 ± 0.11 | 0.2 ± 0.1 |
| Cyclazocine | 1.81 ± 0.67 | 4.59 ± 0.58 |
| Nalbuphine | 3.47 ± 1.18 | 8.5 ± 5.39 |
| Butorphanol | 2.92 ± 1.55 | 2.75 ± 0.13 |
| Diprenorphine | 2.2 ± 0.71 | 3.0 ± 0.86 |
| Buprenorphine | 1.8 ± 0.93 | 2.13 ± 0.27 |
| Other | ||
| Morphine, CTAP, DAMGO, oxymorphone, oxycodone, morphine-6β-glucuronide, β-endorphin, codeine, meperidine, [d-Ala2,d-Leu5]-enkephalin (DADLE), DPDPE, SNC80, U50,488H, dynorphin A, α-neoendorphin, orphanin FQ/nociceptin (OFQ/N), OFQ/N(1\x{2013}11), J-113397, JTC801, (+)-SKF10,047, (+) pentazocine, and haloperidol | Inactive (>1,000) | |
125I-BNtxA competition studies were carried out in mice brain homogenates from triple-KO and WT mice with blockers to prevent binding to traditional mu, kappa1, and delta opioid receptors as described in Materials and Methods.