TY - JOUR
T1 - Effects of U-50488H, a selective κ-analgesic, on the minimum anesthetic concentration (MAC) of halothane in the rat
AU - Althaus, J. S.
AU - VonVoigtlander, P. F.
AU - DiFazio, C. A.
AU - Miller, E. D.
PY - 1987/1/1
Y1 - 1987/1/1
N2 - The effects of U-50488H, a selective κ-analgesic, on the minimum anesthetic concentration (MAC) of an inhalational agent (halothane) were studied in the rat. U-50488H was given subcutaneously in doses of 3, 10, and 30 mg/kg body weight. The maximal MAC reduction was about 60%. The potency ratio of U-50488H to morphine in this model was comparable with potency ratios in other analgesic assays. In separate experiments, the percent reduction in halothane MAC with U-50488H at 30 mg/kg was determined during the infusion of naloxone (5 μg·kg-1·min-1 and 1 mg·kg-1·min-1) at doses shown to have reversed a 70% reduction in MAC by 10 mg/kg of morphine. Only when naloxone was infused at 1 mg·kg-1·min-1 was there a significant reversal of the U-50488H-induced reduction in halothane MAC. This observation suggests that the reduction in MAC of halothane with U-50488H was not mediated by a μ-receptor. In conclusion, through the use of a selective pharmacologic tool that stimulates κ-receptors we have demonstrated potential utility of κ-analgesics as supplements to general anesthesia.
AB - The effects of U-50488H, a selective κ-analgesic, on the minimum anesthetic concentration (MAC) of an inhalational agent (halothane) were studied in the rat. U-50488H was given subcutaneously in doses of 3, 10, and 30 mg/kg body weight. The maximal MAC reduction was about 60%. The potency ratio of U-50488H to morphine in this model was comparable with potency ratios in other analgesic assays. In separate experiments, the percent reduction in halothane MAC with U-50488H at 30 mg/kg was determined during the infusion of naloxone (5 μg·kg-1·min-1 and 1 mg·kg-1·min-1) at doses shown to have reversed a 70% reduction in MAC by 10 mg/kg of morphine. Only when naloxone was infused at 1 mg·kg-1·min-1 was there a significant reversal of the U-50488H-induced reduction in halothane MAC. This observation suggests that the reduction in MAC of halothane with U-50488H was not mediated by a μ-receptor. In conclusion, through the use of a selective pharmacologic tool that stimulates κ-receptors we have demonstrated potential utility of κ-analgesics as supplements to general anesthesia.
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U2 - 10.1213/00000539-198705000-00003
DO - 10.1213/00000539-198705000-00003
M3 - Article
C2 - 3578846
AN - SCOPUS:0023214358
SN - 0003-2999
VL - 66
SP - 391
EP - 394
JO - Anesthesia and analgesia
JF - Anesthesia and analgesia
IS - 5
ER -