[3H]U-69593 a highly selective ligand for the opioid kappa receptor.
The selective kappa agonist U-50488 was recently discovered and characterized. In this study, the receptor binding properties of [3H]U-69593, an analog of U-50488, were characterized. [3H]U-69593 binds with high affinity (3 nM) to membranes prepared from guinea pig, mouse and rat brain. The number of kappa binding sites comprise only 13%, 9% and 4% of the total opioid sites, respectively. The benzmorphans, dynorphin, and compounds structurally related to U-50488 have high affinity for this kappa site.
Lahti
R A
RA
Mickelson
M M
MM
McCall
J M
JM
Von Voigtlander
P F
PF
D000700:Analgesics / Q000378:metabolism*; D000818:Animals; D044482:Benzeneacetamides; D001575:Benzomorphans / Q000378:metabolism; D001921:Brain / Q000378:metabolism; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D051379:Mice; D009270:Naloxone / Q000378:metabolism; D011759:Pyrrolidines / Q000378:metabolism*; D051381:Rats; D011957:Receptors, Opioid / Q000378:metabolism*; D017473:Receptors, Opioid, kappa
D000700:Analgesics; D044482:Benzeneacetamides; D001575:Benzomorphans; D008024:Ligands; D011759:Pyrrolidines; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D009270:Naloxone; C027247:MR 2266; C045444:U 69593