Peripheral kappa 1-opioid receptor-mediated analgesia in mice.
When injected directly into the tail, U50,488H is a potent analgesic in the tailflick assay (ED50 3.1 micrograms). The analgesic activity is lost if the radiant heat is focused 1 cm away from the site of injection. The kappa 1-opioid receptor antagonist nor-binaltorphimine given systemically reverses the local analgesic response of U50,488H, but the antagonist is 100-fold more potent when injected directly into the tail. Intrathecal antisense treatment with a probe targeting the mRNA encoding the kappa 1-opioid receptor blocks the local analgesic actions of U50,488H in the tail, suggesting that U50,488H is acting on dorsal ganglia neurons.
Kolesnikov
Y
Y
Cotzias Laboratory of Neuro-Oncology, New York, NY 10021, USA.
Jain
S
S
Wilson
R
R
Pasternak
G W
GW
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D008297:Male; D051379:Mice; D011759:Pyrrolidines / Q000494:pharmacology*; D012333:RNA, Messenger / Q000378:metabolism; D017473:Receptors, Opioid, kappa / Q000187:drug effects* / Q000235:genetics / Q000502:physiology
D000700:Analgesics; D011759:Pyrrolidines; D012333:RNA, Messenger; D017473:Receptors, Opioid, kappa; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer