RWJ-394674
- In general: legal
- N,N-diethyl-4-((8-phenethyl-8-azabicyclo[3.2.1]oct-3-ylidene)phenylmethyl)benzamide
- 10205965
- 23158278
- ChEMBL68113
- Interactive image
- CCN(CC)C(=O)c1ccc(cc1)C(=C2C[C@H]3CC[C@@H](C2)N3CCc4ccccc4)c5ccccc5
- InChI=1S/C33H38N2O/c1-3-34(4-2)33(36)28-17-15-27(16-18-28)32(26-13-9-6-10-14-26)29-23-30-19-20-31(24-29)35(30)22-21-25-11-7-5-8-12-25/h5-18,30-31H,3-4,19-24H2,1-2H3/b32-29-/t30-,31+/m1/s1
- Key:ZJOPBPNTQRUJNM-BPVGFELESA-N
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 of 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
- ^ Codd EE, Carson JR, Colburn RW, Dax SL, Desai-Krieger D, Martinez RP, et al. (September 2006). "The novel, orally active, delta opioid RWJ-394674 is biotransformed to the potent mu opioid RWJ-413216". The Journal of Pharmacology and Experimental Therapeutics. 318 (3): 1273–9. doi:10.1124/jpet.106.104208. PMID 16766719. S2CID 13165519.
- v
- t
- e
(MOR)
(DOR)
(KOR)
(NOP)
Agonists |
|
---|---|
Antagonists |
|
- Enkephalinase inhibitors: Amastatin
- BL-2401
- Candoxatril
- D -Phenylalanine
- Dexecadotril (retorphan)
- Ecadotril (sinorphan)
- Kelatorphan
- Racecadotril (acetorphan)
- RB-101
- RB-120
- RB-3007
- Opiorphan
- Selank
- Semax
- Spinorphin
- Thiorphan
- Tynorphin
- Ubenimex (bestatin)
- Propeptides: β-Lipotropin (proendorphin)
- Prodynorphin
- Proenkephalin
- Pronociceptin
- Proopiomelanocortin (POMC)
- Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)
This analgesic-related article is a stub. You can help Wikipedia by expanding it. |
- v
- t
- e