emapunil
Emapunil is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO. This protein has multiple functions, among which is regulation of steroidogenesis, particularly the production of neuroactive steroids such as allopregnanolone in the brain. In both animal and human trials, emapunil produced fast acting anxiolytic and anti-panic effects, without producing sedation or withdrawal symptoms following cessation of use. Emapunil is also used in its 11C radiolabelled form to map the distribution of TSPO receptors in the brain. — Wikipedia
Clinical trial activity
7 trials · 4 clinical orgs · 0 marketing orgs
Earliest trial started Mar 1, 2005 (NCT00108836)
Timeline
Indications
Mechanism of action
- Translocator proteinAGONIST
TSPO agonist
Chemistry & pharmacology
SMILES
CCN(Cc1ccccc1)C(=O)Cn1c(=O)n(C)c2cnc(-c3ccccc3)nc21- Mol. weight
- 401.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaEmapunil ↗
- ChEMBLCHEMBL513922 ↗
Also known as
- ac-5216
- ac-5216
- ac-5216
- emapunil
- emapunil
- emapunil
- emapunil
- n-benzyl-n-ethyl-2-(7,8-dihydro-7-methyl-8-oxo-2-phenyl-9h-purin-9-yl)acetamide
- xbd173
- xbd173
- xbd173
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07191821 | Phase 2 | Aug 8, 2025 | Imperial College London |
| NCT06643013 | N/A | Oct 31, 2024 | Imperial College London |
| NCT06035861 | N/A | Nov 1, 2023 | Imperial College London |
| NCT03850301 | N/A | Apr 1, 2018 | Imperial College London |
| NCT02181582 | Phase 1 | Jun 24, 2014 | National Institute of Mental Health (NIMH) |
| NCT02086240 | N/A | Mar 1, 2014 | University of London |
| NCT00108836 | Phase 2 | Mar 1, 2005 | Novartis |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Imperial College London | Academic/Hospital | 4 | 4 | 2 | 2018 |
| National Institute of Mental Health (NIMH) | Government | 1 | 1 | 1 | 2014 |
| Novartis | For profit | 1 | 1 | 1 | 2005 |
| University of London | Academic/Hospital | 1 | 1 | 1 | 2014 |