buprenorphine
A derivative of the opioid alkaloid THEBAINE that is a more potent and longer lasting analgesic than MORPHINE. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use.
Ligand Summary
UNII: 40D3SCR4GZ
PubChem: 45265653
PubChem: 644073
Guide to Pharmacology: 1670
ChEMBL: CHEMBL511142
ChEMBL: CHEMBL1200401
ChEMBL: CHEMBL560511
DrugCentral: 434
LyCHI: 1MYL2TZ39DL2
Target Activities
OPRM1
Mu-type opioid receptor
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.77 | J. Med. Chem., (2001) 44:21:3378 | ||||
Ki | 8.8 | J. Med. Chem., (2015) 58:24:9754 | ||||
- | 8.80000019 | |||||
Ki | 8.29 | PARTIAL AGONIST | ||||
OPRK1
Kappa-type opioid receptor
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.92 | J. Med. Chem., (2001) 44:21:3378 | ||||
Ki | 9.01 | ANTAGONIST | ||||
OPRD1
Delta-type opioid receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.05 | J. Med. Chem., (2001) 44:21:3378 | ||||
OPRL1
Nociceptin receptor
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.11 | |||||