FSL0707

Structure

• InChI=1S/C19H21NO4/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11/h2-4,14,17,21,23H,1,5-10H2/t14-,17-,18+,19-/m1/s1
• InChIKey=UZHSEJADLWPNLE-DQEVTTJGSA-N

Synonyms

• 465-65-6
• Naloxone

Origin

Chemically synthesized

Biological activities

Suppression of the opiate overdose effects

Therapeutic

Antinarcotic

Target

Opioid receptors
Cyclic AMP-responsive element-binding protein 1

Assay information

A narcotic atagonist to treat narcotic overdose
Binding to all of three opioid receptors (μ, κ and δ)
Strongest binding is to the μ-receptor (K_i for μ =1.8 nM, for κ = 17.2 nM, for δ = 27.0 nM)

References

• Magnan J, Paterson SJ, Tavani A, Kosterlitz HW
  The binding spectrum of narcotic analgesic drugs with different agonist and antagonist properties.
  Naunyn Schmiedebergs Arch Pharmacol, 319(3): 197-205 (1982)  6125900
• Ann. Intern. Med., 85: 765-768 (1976)
• Lewenstein Mozes Juda, Gardens Kew, Fishman Jack
  (1966). Morphine derivative. US3254088 A.