Table 1.
Compounds targeting the N/OFQ system, relative developmental stage and effects on addiction.
| Agonist | Chemical entity | Effects on drug taking and relapse | Dev. phase | Ref. |
|---|---|---|---|---|
| N/OFQ | peptidic | ↓ Alcohol intake | Preclinic | 36, 38 |
| Ro 64-6198 | small molecule | ↓ ↑ Alcohol intake | Preclinic | 70, 82 |
| Ro 64-6570 | small molecule | Not tested | Preclinic | 71 |
| W212393 | small molecule | Not tested | Preclinic | 72 |
| GRT6005 | small molecule | Not tested | Clinic | NCT01725087 |
| SCH 655842 | small molecule | Not tested | Preclinic | 74 |
| SCH 221510 | small molecule | Not tested | Preclinic | 75 |
| UFP-112 | peptidic | ↓ Alcohol intake | Preclinic | 70 |
| UFP-102 | peptidic | ↓ Alcohol intake | Preclinic | 70 |
| OS-462 | peptidic | ↓ Alcohol intake | Preclinic | 70 |
| Buprenorphine * | small molecule | ↓ Alcohol intake | Clinic | 46 |
| SCH 486757 | small molecule | Not tested | Clinic | 73 |
| NCT00230230 | ||||
| Antagonist | ||||
| UFP-101 | peptidic | — Alcohol intake | Preclinic | 46 |
| J113397 | small molecule | Not tested | Preclinic | 76 |
| NiK-21273 | small molecule | Not tested | Preclinic | 77 |
| Compound 24 | small molecule | Not tested | Preclinic | 78 |
| SB-612111 | small molecule | Not tested | Preclinic | 79 |
| Nphe | peptidic | — Alcohol intake | Preclinic | 80 |
| GF-4 | peptidic | Not tested | Preclinic | 81 |
*
Buprenorphine-induced alcohol drinking reduction is mediated by NOP.