norbuprenorphine
Small moleculeexperimental
Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine. It is a μ-opioid, δ-opioid, and nociceptin receptor full agonist, and a κ-opioid receptor partial agonist. In rats, unlike buprenorphine, norbuprenorphine produces marked respiratory depression but with very little antinociceptive effect. In explanation of these properties, norbuprenorphine has been found to be a high affinity P-glycoprotein substrate, and in accordance, shows very limited blood-brain-barrier penetration. — Wikipedia
Clinical trial activity
1 trials · 2 clinical orgs · 0 marketing orgs
Phase 1
1
Phase 2
0
Phase 3
0
Phase 4
0
Earliest trial started Jan 1, 2016 (NCT02666001)
Timeline
2010s
- Jan 1, 2016
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Delta opioid receptorAGONIST
OPRD1 agonist
- Nociceptin receptorAGONIST
OPRL1 agonist
- Mu opioid receptorAGONIST
OPRM agonist
Chemistry & pharmacology
Loading structure…
SMILES
CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1)[C@H]2O5- Mol. weight
- 413.56 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaNorbuprenorphine ↗
- ChEMBLCHEMBL1743323 ↗
Also known as
- des(cyclopropylmethyl)buprenorphine
- n-desalkylbuprenorphine
- norbuprenorphine
- norbuprenorphine
- norbuprenorphine
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02666001 | Phase 1 | Jan 1, 2016 | GlaxoSmithKline, ViiV Healthcare |
Showing 1 of 1 trials
Page 1 / 1
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 1 | 0 | 1 | 2016 |
| ViiV Healthcare | For profit | 1 | 1 | 1 | 2016 |
2 organizations
Page 1 / 1