Table 5:
Genes reported related to opioid dependence.
| Gene symbol | Finding | Citations |
|---|---|---|
| ABAT, ALDH5A1 | Valproic acid, an inhibitor of the ABAT protein and ALDH5A1 protein, is in Phase IV to treat opiate dependence | [93] |
| ADRA1A, ADRA1B, ADRA1D, ADRA2A, ADRA2B, ADRA2C | Paliperidone, an antagonist of ADRA1A, ADRA1B, ADRA1D, ADRA2A, ADRA2B, and ADRA2C proteins, is in Phase III to treat heroin dependence | [132] |
| CACNA2D1, CACNA2D2 | Gabapentin, an inhibitor of human CACNA2D1 and CACNA2D2 proteins, is in Phase IV as a treatment for opioid dependence | [133] |
| DRD2 | Buspirone, an agonist of human DRD2 protein, is in Phase IV as a treatment for heroin dependence | [103] |
| DRD2, DRD3, DRD4 | Paliperidone, an antagonist of human DRD2, DRD3, and DRD4 proteins, is in Phase III as a treatment for heroin dependence | [132] |
| GABRA1, GABRA3, GABRA4, GABRA5, GABRA6, GABRB1, GABRB2, GABRE, GABRG1, GABRG2, GABRG3, GABRP | Isoniazid, an inhibitor of human GABRA1, GABRA3, GABRA4, GABRA5, GABRA6, GABRB1, GABRB2, GABRE, GABRG1, GABRG2, GABRG3, and GABRP proteins, is in Phase IV in combination with naltrexone as a treatment for opioid dependence | [134–135] |
| GABRB3 | Isoniazid, an inhibitor of human GABRB3 protein, is in Phase IV in combination with naltrexone as a treatment for opioid dependence | [134–135] |
| Mutant human GABRB3 (SNP substitution [rs7165224]) is associated with heroin addiction in humans (p=0.01). | [136] | |
| GAD2 | Valproic acid, an inhibitor of human GAD2 protein, is in Phase IV in combination with buprenorphine as a treatment for opiate dependence | [89] |
| GRIN1, GRIN2B, GRIN2A, GRIN2C, GRIN2D, GRIN3A, GRIN3B | Ketamine, an antagonist of human GRIN1, GRIN2B, GRIN2A, GRIN2C, GRIN2D, GRIN3A, and GRIN3B proteins, is in Phase IV as a treatment for opiate dependence | [137] |
| Memantine, an antagonist of human GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D, GRIN3A, and GRIN3B proteins, is in Phase II/III as a treatment for opioid dependence | [138] | |
| Memantine, an antagonist of human GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D, GRIN3A, and GRIN3B proteins, is being tested in combination with Vivitrol [naltrexone] as a treatment for opioid dependence | [139] | |
| GRIN3A, HTR3A | Methadone, an antagonist of human GRIN3A and HTR3A proteins and mu-opioid receptor, has been approved as a treatment for opioid dependence | [140] |
| HRH1 | Mirtazapine, a blocker of human HRH1, HTR2A, HTR2B, and HTR2C proteins, is in Phase III as a treatment for heroin dependence | [141] |
| Paliperidone, an antagonist of human HRH1, HTR2A, and HTR2C proteins, is in Phase III as a treatment for heroin dependence | [142] | |
| HTR1A | Buspirone, an agonist of human HTR1A proteins, is in Phase IV as a treatment for heroin dependence | [103] |
| HTR2A, HTR2C | Mirtazapine, a blocker of human HRH1, HTR2, HTR2A, HTR2B, and HTR2C proteins, is in Phase III as a treatment for heroin dependence | [141] |
| Paliperidone, an antagonist of human HRH1, HTR2A, and HTR2C proteins, is in Phase III as a treatment for heroin dependence | [142] | |
| Buspirone, an agonist of human HTR1A, HTR2A, HTR2B, and HTR2C proteins, is in Phase IV as a treatment for heroin dependence | [103] | |
| HTR2B, | Mirtazapine, a blocker of human HRH1, HTR2, HTR2A, HTR2B, and HTR2C proteins, is in Phase III as a treatment for heroin dependence | [141] |
| Buspirone, an agonist of human HTR1A, HTR2A, HTR2B, and HTR2C proteins, is in Phase IV as a treatment for heroin dependence | [103] | |
| OPRM1 | Mutant human OPRM1 (c.118A>G [germline] (rs1799971)) is observed to carry susceptibility to opioid dependence type 1 in humans | [55] |
| Naloxone, an antagonist of human OPRM1 protein, has been approved in the combination Cassipa [buprenorphine/naloxone] (maintenance) as a treatment for opioid dependence | ||
| Naltrexone, an antagonist of human OPRM1 protein, is in Phase IV as a treatment for opioid dependence | [56, 143] | |
| Buprenorphine, antagonist of OPRM1 protein, and naloxone in combination are in Phase IV as a treatment for opioid dependence. | [144] | |
| Hydromorphone, an agonist of human OPRM1 protein, is in Phase III as a component of a treatment for opioid dependence | [145–146] | |
| Buprenorphine, an antagonist of OPRM1 protein, and naloxone in combination are in Phase III as a treatment for heroin dependence | [147–155] | |
| OPRD1, OPRK1 | Naloxone, an antagonist of human OPRD1 and OPRK1 proteins, has been approved as a part of the combination drug Cassipa [buprenorphine/naloxone] (maintenance) as a treatment for opioid dependence | [147] |
| Naltrexone, an antagonist of human OPRD1 and OPRK1 proteins, is in Phase IV as a treatment for opioid dependence | [56, 143] | |
| Buprenorphine, an agonist of human OPRD1 and antagonist of OPRK1 proteins, and naloxone in combination are in Phase IV as a treatment for opioid dependence | [144] | |
| Hydromorphone, an agonist of human OPRD1 and OPRK1 proteins, is in Phase III as a component of a treatment for opioid dependence | [145–146] | |
| Buprenorphine, agonist of human OPRD1 and antagonist of OPRK1 protein, and naloxone and a combination are in Phase III as a treatment for heroin dependence | [147–155] | |
| SIGMAR1 | Naloxone, an antagonist of human SIGMAR1 protein, has been approved as a part of the combination drug Cassipa [buprenorphine/naloxone] (maintenance) as a treatment for opioid dependence | [147] |
| Naltrexone, an antagonist of human SIGMAR1 protein, is in Phase IV as a treatment for opioid dependence | [56, 143] | |
| Hydromorphone, an agonist of human SIGMAR1 protein, is in Phase III as a component of a treatment for opioid dependence | [145–146] | |
| SLC6A2, SLC6A3, SLC6A4 | Bupropion, an inhibitor of human SLC6A2, SLC6A3, and SLC6A4 proteins, is in Phase III as a component of a treatment for opioid dependence | [156] |