RWJ-394674
 |
|
| Systematic (IUPAC) name | |
|---|---|
|
N,N-diethyl-4-((8-phenethyl-8-azabicyclo[3.2.1]oct-3-ylidene)phenylmethyl)benzamide
|
|
| Legal status | |
| Legal status |
|
| Identifiers | |
| PubChem | CID 10205965 |
| ChemSpider | 23158278 |
| ChEMBL | CHEMBL68113 |
| Chemical data | |
| Formula | C33H38N2O |
| Molar mass | 478.667 g/mol |
| 3D model (Jmol) | Interactive image |
|
|
|
|
| (verify) | |
RWJ-394674 is a drug that is used in scientific research. It is a potent, orally active analgesic drug that produces little respiratory depression. RWJ-394674 itself is a potent and selective agonist for δ-opioid receptors, with a Ki of 0.24 nM at δ and 72 nM at μ. However once inside the body, RWJ-394674 is dealkylated to its monodesethyl metabolite RWJ-413216, which is a potent agonist at the μ-opioid receptor and has less affinity for δ (Ki 0.26 nM at μ, 46.7 nM at δ). The effect of RWJ-394674 when administered in vivo thus produces potent agonist effects at both μ and δ receptors through the combined actions of the parent drug and its active metabolite, with the δ-agonist effects counteracting the respiratory depression from the μ-opioid effects, and the only prominent side-effect being sedation.[1]
References[edit]
- ^ Codd EE, Carson JR, Colburn RW, Dax SL, Desai-Krieger D, Martinez RP, McKown LA, Neilson LA, Pitis PM, Stahle PL, Stone DJ, Streeter AJ, Wu WN, Zhang SP. The novel, orally active, delta opioid RWJ-394674 is biotransformed to the potent mu opioid RWJ-413216. Journal of Pharmacology and Experimental Therapeutic. 2006 Sep;318(3):1273-9. PMID 16766719
 |
This analgesic-related article is a stub. You can help Wikipedia by expanding it. |
