Relative affinities of the quaternary narcotic antagonist, N-methyl levallorphan (SR 58002), for different types of opioid receptors.
The relative affinities for different subtypes of opioid receptors (mu, kappa and delta) of the peripheral narcotic antagonist N-methyl levallorphan (SR 58002) have been studied in two in vitro smooth muscle systems (guinea-pig ileum and rabbit vas deferens) and by binding studies (guinea-pig brain and cerebellum membranes) using selective tritiated ligands. All the evidence obtained indicates that SR 58002 is a pure antagonist with relative affinity for mu receptors vs kappa and delta superior to that of the parent tertiary compound, levallorphan.
Bianchetti
A
A
Dragonetti
M
M
Giudice
A
A
Tarantino
A
A
Ferrarese
N
N
Manara
L
L
Appelmans
N
N
Simon
E J
EJ
D000818:Animals; D001667:Binding, Competitive; D002531:Cerebellum / Q000378:metabolism; D006168:Guinea Pigs; D007082:Ileum / Q000378:metabolism; D066298:In Vitro Techniques; D007977:Levallorphan / Q000031:analogs & derivatives* / Q000378:metabolism; D008297:Male; D009294:Narcotics / Q000378:metabolism; D011817:Rabbits; D011957:Receptors, Opioid / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D014649:Vas Deferens / Q000378:metabolism
D009294:Narcotics; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D007977:Levallorphan; C045482:N-methyllevallorphan