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CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C35H49NO10 |
Molar mass | 643.774 g·mol−1 |
3D model ( JSmol) | |
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Buprenorphine-3-glucuronide (B3G) is a major active metabolite of the opioid modulator buprenorphine. [1] It has affinity for the μ-opioid receptor (Ki = 4.9 (± 2.7) pM), δ-opioid receptor (Ki = 270 nM), and nociceptin receptor (Ki = 36 μM), but not for the κ-opioid receptor. [1] Whether B3G acts as an agonist or antagonist of each of the former three respective sites has yet to be determined. [2] In rats, at the doses assayed, B3G has been found to produce a small degree of antinociception, and similarly to buprenorphine in these assays, has not been found to produce sedation, reduce locomotion, or decrease respiratory rate. [1] Of all of the active metabolites of buprenorphine, B3G is thought to be the most similar to the parent drug. [1] Unlike norbuprenorphine, but similarly to buprenorphine (and norbuprenorphine-3-glucuronide), B3G is not a substrate for P-glycoprotein, and hence may cross the blood-brain-barrier significantly. [2]
![]() | |
Clinical data | |
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ATC code |
|
Identifiers | |
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
CompTox Dashboard ( EPA) | |
Chemical and physical data | |
Formula | C35H49NO10 |
Molar mass | 643.774 g·mol−1 |
3D model ( JSmol) | |
| |
|
Buprenorphine-3-glucuronide (B3G) is a major active metabolite of the opioid modulator buprenorphine. [1] It has affinity for the μ-opioid receptor (Ki = 4.9 (± 2.7) pM), δ-opioid receptor (Ki = 270 nM), and nociceptin receptor (Ki = 36 μM), but not for the κ-opioid receptor. [1] Whether B3G acts as an agonist or antagonist of each of the former three respective sites has yet to be determined. [2] In rats, at the doses assayed, B3G has been found to produce a small degree of antinociception, and similarly to buprenorphine in these assays, has not been found to produce sedation, reduce locomotion, or decrease respiratory rate. [1] Of all of the active metabolites of buprenorphine, B3G is thought to be the most similar to the parent drug. [1] Unlike norbuprenorphine, but similarly to buprenorphine (and norbuprenorphine-3-glucuronide), B3G is not a substrate for P-glycoprotein, and hence may cross the blood-brain-barrier significantly. [2]