Enadoline Explained

Enadoline is a drug which acts as a highly selective κ-opioid agonist.

In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A.^[1]

It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist. There was mention of its potential in treating comatose head injury or stroke victims, where that type of side effect would be immaterial.^[2]

Potency

When enadoline was first reported in 1990, it was "the most potent κ-selective analgesic ever reported ... 25 times more potent than morphine and 17 times more potent than U-62066".^[3]

See also

• U-69,593
• U-50,488
• U-77891
• AH-7921
• bromadoline

Notes and References

1. Walsh SL, Strain EC, Abreu ME, Bigelow GE . Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans . Psychopharmacology . 157 . 2 . 151–162 . September 2001 . 11594439 . 10.1007/s002130100788 . 10507758 .
2. Barber A, Gottschlich R . Novel developments with selective, non-peptidic kappa-opioid receptor agonists . Expert Opinion on Investigational Drugs . 6 . 10 . 1351–1368 . October 1997 . 15989506 . 10.1517/13543784.6.10.1351 .
3. Halfpenny PR, Horwell DC, Hughes J, Hunter JC, Rees DC . Highly selective kappa-opioid analgesics. 3. Synthesis and structure-activity relationships of novel N-[2-(1-pyrrolidinyl)-4- or -5-substituted-cyclohexyl]arylacetamide derivatives . Journal of Medicinal Chemistry . 33 . 1 . 286–291 . January 1990 . 2153208 . 10.1021/jm00163a047 .