Table 1.
Targets of Interest for Alcohol Dependence Medications
| Receptors | Representative Compounds | Status |
|---|---|---|
| 5–HT3* | ondansetron | Preclinical, clinical |
| 5–HT2* | olanzapine | Preclinical, clinical |
| adenosine A2a | DMPX | Preclinical |
| adrenergic α1* | prazosin | Preclinical, clinical |
| AMPA/GABAa receptor* | topiramate | Preclinical, clinical |
| CRF1 | antalarmin, MTIP, Pexacerfont, GSK561679 | Preclinical, clinical |
| GABA–A | RY 023 | Preclinical |
| GABA–B* | baclofen, CGP7930, GS39783, BHF177 | Preclinical, clinical |
| GLT1* | ceftriaxone | Preclinical |
| mGluRs | MTEP | Preclinical |
| nAChRs* | varenicline, CP–601932 | Preclinical, clinical |
| NK1* | LY686017, Aprepitant | Preclinical, clinical |
| NMDA Receptors* | neramexane, memantine | Preclinical, clinical |
| NOP | OS–462, UFP–102, UFP–112 | Preclinical |
| NPS receptor | NCG–0018568403 | Preclinical |
| NPY1, NPY2 | BIIE0246, JNJ–31020028, | Preclinical |
| opioid receptors* | nalmefene, naltrexone | Preclinical, clinical |
| DOR | SoRI–9409, TAN–67 | Preclinical |
| KOR | Nor–BNI | Preclinical |
| OX1, OX2 | SB–334867, JNJ–10397049 | Preclinical |
| P2X4* | Ivermectin | Preclinical |
| Vasopressin 1b | nelivaptan (SSR 149415) | Preclinical |
| Other Targets | ||
| ALDH–2 | CVT–10216 | Preclinical |
| GDNF | noribogaine | Preclinical |
| Glycine transporter, GlyT-1 | Org 25935 | Preclinical, clinical |
| HDAC* | SAHA, trichostatin A | Preclinical |
| L–type calcium channel auxiliary subunit, GABA modulator | gabapentin, pregabalin | Preclinical, clinical |
| mTORC1* | rapamycin, | Preclinical |
| Neuroimmune modulation | minocycline, ibudilast, pioglitazone | Preclinical |
| PDE4* | rolipram | Preclinical |
| PKC–epsilon | proprietary | Preclinical |
| Serotonin–norepinephrine transporter | duloxetine | Preclinical, clinical |
| Sigma–1 receptor | NE-100 | Preclinical |
5-HT, 5–Hydroxytryptamine ; ADLH, aldehyde dehydrogenase; AMPA, α–amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid; CB, cannabinoid; CRF, corticotrophin releasing factor; DOR, d-opioid receptor; GABA, gamma–aminobutyric acid; GDNF, glial derived neurotrophic factor; GLT1, glutamate transporter 1; HDAC, Histone deacetylase; KOR, δ–opioid receptor; mGluR, metabotropic glutamate receptor; MOR, μ–opioid receptor; mTOR1, mammalian target of rapamycin complex 1; nAChR, nicotinic acetylcholine receptors; NK, neurokinin; NOP, opioid receptor-like 1; NPS, Neuropeptide S; NPY, neuropeptide Y; OX, orexin receptor; P2X4, purinergic receptor P2X, ligand–gated ion channel, 4; PDE: phosphodiesterase; PKC, protein kinase C.
FDA-approved compounds available for this target.