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Rwj-394674

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Title: Rwj-394674  
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Rwj-394674

RWJ-394674
Systematic (IUPAC) name
N,N-diethyl-4-((8-phenethyl-8-azabicyclo[3.2.1]oct-3-ylidene)phenylmethyl)benzamide
Clinical data
Legal status
  • Legal
Identifiers
PubChem CID:
Chemical data
Formula C33H38N2O
Molecular mass 478.667 g/mol
 YesY   

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

  1. ^ 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



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