Table 1.
A short list of Sig-1R ligands (agonists and antagonists).
| Agonists | Refs. | Other Activities |
|---|---|---|
| N,N-Dimethyltryptamine (DMT) | [3, 172, 173] | 5HT2A receptor agonist |
| (+)-N-allylnormetazocine ((+)-SKF 10,047) | [51] | NMDA receptor ligand |
| 2-(4-morpholino)ethyl-1-phenylcyclohexane-1-carboxylate (PRE-084) | [23, 174] | – |
| 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl) piperazine (SA 4503, cutamesine) | [175] | – |
| 4-phenyl-1-(4-phenylbutyl)piperidine (PPBP) | [176] | nNOS inhibition |
| 1-(2,8-Dimethyl-1-thia-3,8-diazaspiro(4,5)dec-3-yl)-3-(1H-indol-3-yl)propan-1-one (AF710B) | [123] | allosteric M1 agonist |
| Dehydroepioandrosterone (DHEA) | [177] | neurosteroid, nuclear receptors |
| Donepezil | [128, 178, 179] | cholinesterase inhibitor |
| Amitriptyline | [180] | neurotransmitter reuptake blocker |
| Fluvoxamine | [23, 36, 181, 182] | 5HT reuptake inhibitor |
| Memantine | [183] | NMDAR antagonist |
| Ifenprodil | [184] | NMDAR antagonist, α-1 antagonist |
| (+)-Pentazocine | [23, 185, 186] | – |
| Cocaine | [23, 187] | neurotransmitter reuptake blocker |
| Dextromethorphan (DEX) | [30, 188] | NMDAR allosteric antagonist |
| Antagonists | ||
| N-(2-(3,4-dichlorophenyl)-N-methyl-2-(dimethylamino)ethylamine (BD 1047) | [189] | β-adrenoreceptor ligand |
| 1-(2-(3,4-dichlorophenyl)ethyl)-4-methylpiperazine (BD 1063) | [189] | – |
| 4-Methoxy-3-(2-phenylethoxy)- N,N-dipropylbenzeneethaneamine (NE-100) |
[23] | – |
| Progesterone | [23] | neurosteroid, progestogen |
| Haloperidol | [23] | D2 and D3 antagonist |
| Verapamil | [190] | Ca2+-antagonist, slow channel blocker |
| Sertraline | [60] | 5HT reuptake inhibitor |