Use of methadone metabolites for treatment of anxiety and depression
US11278522B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 13, 2020 |
| Grant date | Mar 22, 2022 |
| Priority date | — |
| Expiry date | Jul 13, 2040 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P25/24
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Previous studies (Xiao et al., 2001) have identified two metabolites of methadone, EMDP (2-ethyl-5-methyl-3,3-diphenyl-1-pyrroline) and EDDP (2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine), which are considered to be inactive at opiate receptors, as relatively potent noncompetitive channel blockers of α3β4 nAChRs. We have now evaluated these compounds in rats and mice in preclinical behavioral models predictive of potential anxiolytic and antidepressant efficacy. We found that EMDP, but not EDDP, displayed robust effects predictive of anxiolytic and antidepressant efficacy without significant effects on locomotor activity. Moreover, EMDP at behaviorally active doses, unlike mecamylamine, did not produce eyelid ptosis, suggesting it may produce fewer autonomic side effects than mecamylamine. Thus, the methadone metabolite EMDP may represent a novel therapeutic avenue for the treatment of some affective disorders.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.