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Dezocine
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Cat No: 34093
Biochemicals
- Receptor Pharmacology
Dezocine is a partial agonist of the µ- and κ-opioid receptors.{58497} It is selective for µ- and κ-opioid receptors (Kis = 1.46 and 22.01 nM, respectively) over the δ-opioid receptor (Ki = 398.6 nM). Dezocine inhibits the norepinephrine transporter (...
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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
- (5R,11S,13S)-amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecen-3-ol
Correlated keywords:
- 58918-18-6 Wy16225 (-)-Dezocine
Product Overview:
Dezocine is a partial agonist of the µ- and κ-opioid receptors.{58497} It is selective for µ- and κ-opioid receptors (Kis = 1.46 and 22.01 nM, respectively) over the δ-opioid receptor (Ki = 398.6 nM). Dezocine inhibits the norepinephrine transporter (NET) and serotonin transporter (SERT) with Ki values of 0.001 and 109 nM, respectively.{58498} It stimulates [35S]GTPγS binding to CHO membranes expressing the human µ- and κ-opioid receptors with Emax values of 45.8 and 33.6% compared to the µ- and κ-agonists DAMGO and U50,488 H, respectively, when used at a concentration of 10 µM.{58497} It has antinociceptive effects in mice in the acetic acid abdominal constriction test (ED50 = 0.02 mg/kg) and the formalin test (ED50s = 0.4 mg/kg for both phases).{58497} Dezocine (10 mg/kg) increases the latency to tail withdrawal in the tail-flick test in rats.{58499} It also decreases the number of lung metastases in a 4T1 murine mammary cancer model when administered at doses ranging from 0.75 to 2 mg/kg.{58500} Formulations containing dezocine have been used in the treatment of post-operative pain.
Dezocine is a partial agonist of the µ- and κ-opioid receptors.{58497} It is selective for µ- and κ-opioid receptors (Kis = 1.46 and 22.01 nM, respectively) over the δ-opioid receptor (Ki = 398.6 nM). Dezocine inhibits the norepinephrine transporter (NET) and serotonin transporter (SERT) with Ki values of 0.001 and 109 nM, respectively.{58498} It stimulates [35S]GTPγS binding to CHO membranes expressing the human µ- and κ-opioid receptors with Emax values of 45.8 and 33.6% compared to the µ- and κ-agonists DAMGO and U50,488 H, respectively, when used at a concentration of 10 µM.{58497} It has antinociceptive effects in mice in the acetic acid abdominal constriction test (ED50 = 0.02 mg/kg) and the formalin test (ED50s = 0.4 mg/kg for both phases).{58497} Dezocine (10 mg/kg) increases the latency to tail withdrawal in the tail-flick test in rats.{58499} It also decreases the number of lung metastases in a 4T1 murine mammary cancer model when administered at doses ranging from 0.75 to 2 mg/kg.{58500} Formulations containing dezocine have been used in the treatment of post-operative pain.
| Size | 1 mg |
| Shipping | dry ice |
| CAS Number | 53648-55-8 |
| Molecular Formula | C16H23NO |
| SMILES | C[C@@]12C3=CC(O)=CC=C3C[C@H](CCCCC2)[C@@H]1N |
| Molecular Weight | 245,4 |
| Formulation | A solid |
| Purity | ≥95% |
| Custom Code | 2922.29 |
| UNSPSC code | 12352100 |
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