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• W2022254583 abstract "Dose-responsive motor activity induced by systemic injection of the kappa (κ) preferring opioid agonist, U50,488H (1–10 mg/kg, s.c.) in guinea pigs was recenlty reported [Brent P.J. and Bot G. (1992) Psychopharmacology107: 581–590], characterised at the higher doses used (5–10 mg/kg) by sustained postural abnormalities. The effects on the U50,488H-induced, abnormal, motor response of pharmacological manipulation of opioid receptors and sigma (σ) sites was studied. The opiois antagonist naloxone, [5 and 15 mg/kg, subcutaneously (s.c.)], the κ selective antagonist, norbinaltorphimine (NBNI), administered intracerebroventricularly (i.c.v., 20 and 50 nM) 0.5 hr before U50,488H, and the anticonvulsant phenytoin [25 and 50 mg/kg, intraperitoneally (i.p.)] given 1 hr before, attenuated the abnormal postures, whereas naloxone methobromide (15 mg/kg), a quaternary opioid which does not cross the blood-brain barrier, had no significant effect on the movements. In contrast, the drugs with varying affinity for σ binding sites such as 1,3-di(2-tolyl)guanidine (DTG, 10 and 30 mg/kg), haloperidol (1 and 5 mg/kg, s.c.), dextromethorphan (1, 10 and 20 mg/kg, s.c.) and reduced haloperidol (1 mg/kg, s.c.), given 0.5-1 hr before U50,488H, exacerbated the severity of the abnormal motor activity in a dose-related manner by decreasing the latency to onset of maximum obtainable motor response and increasing the duration of the response. In addition, haloperidol (1 and 5 mg/kg, s.c.), dextromethorphan (10 mg/kg, s.c.) and DTG (30 mg/kg, s.c.), given in combination with U50,488H, induced behaviour characterised by marked oral activity. In contrast to the effect of haloperidol, pretreatment with the selective dopamine D-2 antagonist, raclopride (10 mg/kg, s.c.), had no significant effect on the abnormal movements induced by U50,488H, but did induce oral activity. These data indicate the possible involvement of k opioid receptors in the abnormal movement induced by U50,488H, and further demonstrate that there is an interaction between the k receptors and σ sites which can influence the abnormal motor activity." @default.
• W2022254583 created "2016-06-24" @default.
• W2022254583 creator A5075767949 @default.
• W2022254583 date "1993-08-01" @default.
• W2022254583 modified "2023-09-24" @default.
• W2022254583 title "Behavioural effect of pretreatment opioid antagonists and sigma binding site ligands on the abnormal motor response produce by the Kappa opioid agonist U50,488H in guneaa pigs" @default.
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• W2022254583 doi "https://doi.org/10.1016/0028-3908(93)90183-4" @default.
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