Table 2.
Opioid and benzodiazepine receptor binding of 2′-pyridine substituted imidazodiazepines.
| Entry | Name | R1 | R2 | R3 CH3 | KOR 1 % | MOR 1 % | DOR 1 % | BZR 1 % |
KOR (Ki, nM) |
BZR (Ki, nM) |
|---|---|---|---|---|---|---|---|---|---|---|
| 1 | MP-II-068 | HC≡C | iPrO | H | 85 | 0 | 34 | 97 | 550 | 42 |
| 2 | GL-II-06 | Br | EtO | (R) | 79 | 11 | 9 | 81 | 401 | 556 |
| 3 | Hz-166 | HC≡C | EtO | H | 60 | 6 | 49 | n.d. | 3821 | n.d. |
| 4 | GL-II-19 | HC≡C | EtO | (R) | 44 | 17 | 2 | 71 | - 2 | 1143 |
| 5 | MP-III-024 | HC≡C | MeO | H | 43 | 0 | 24 | 81 | - 2 | 277 |
| 6 | GL-II-32 | HC≡C | MeO | (R) | 35 | 32 | 0 | 63 | - 2 | 1427 |
| 7 | GL-II-31 | HC≡C | MeHN | (R) | 23 | 17 | 3 | 72 | - 2 | 1697 |
| 8 | GL-II-51 | Br | HO | (R) | 11 | 0 | 0 | 84 | - 2 | 181 |
| 9 | SR-II-54 | HC≡C | HO | H | 9 | 8 | 1 | 80 | - 2 | 69 |
| 10 | GL-II-30 | HC≡C | HO | (R) | 0 | 20 | 4 | 65 | - 2 | 431 |
1 Percent inhibition at 10,000 nM, 2 dose response was carried out only for compounds with an inhibition of >50%, n.d. = not determined.