RWJ-394,674

drugbox


width = 260
IUPAC_name = N,N-diethyl-4-((8-phenethyl-8-azabicyclo [3.2.1] oct-3-ylidene)phenylmethyl)benzamide
PubChem = 10205965
C = 33 | H = 38 | N = 2 | O = 1
molecular_weight = 478.667 g/mol
smiles = c5ccccc5CCN1C(C4)CCC1CC4=C(c3ccc(cc3)C(=O)N(CC)CC)c2ccccc2
CAS_number =
legal_status = Legal

RWJ-394,674 is a drug which is used in scientific research. It is a potent, orally active analgesic drug, which produces little respiratory depression. RWJ-394,674 itself is a potent and selective agonist for δ-opioid receptors, with a Ki of 0.24nM at δ and 72nM at μ. However once inside the body, RWJ-394,674 is dealkylated to its monodesethyl metabolite RWJ-413,216 which is a potent agonist at the μ-opioid receptor and has less affinity for δ (Ki 0.26nM at μ, 46.7nM at δ). The effect of RWJ-394,674 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. [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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