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Enadoline


Enadoline
Systematic (IUPAC) name
2-(benzofuran-4-yl)-N-methyl-N-((5R,7S,8S)-7- (pyrrolidin-1-yl)-1-oxaspiro[4.5] decan-8-yl)ethanamide
Identifiers
CAS number	124378-77-4
ATC code	?
PubChem	60768
Chemical data
Formula	C₂₄H₃₂N₂O₃
Mol. mass	396.52 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

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

Additional recommended knowledge

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Essential Laboratory Skills Guide

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

It was looked at 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]

References

^ Walsh SL, Strain EC, Abreu ME, Bigelow GE (2001). "Enadoline, a selective kappa opioid agonist: comparison with butorphanol and hydromorphone in humans". Psychopharmacology (Berl.) 157 (2): 151–62. PMID 11594439.
^ Barber A, Gottschlich R (1997). "Novel developments with selective, non-peptidic kappa-opioid receptor agonists". Expert Opin Investig Drugs 6 (10): 1351–68. doi:10.1517/13543784.6.10.1351. PMID 15989506.

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