Route of Administration:
Intraperitoneal
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in rhesus monkeys: When responding was stable, dimethocaine (0.030-1.7 mg/kg/ infusion) was substituted for the cocaine training dose. Dimethocaine administration produced higher response rates compared with that of procaine, and was a more potent reinforcer. Drug effects on behavior were related to DAT occupancy in monkey striatum during neuroimaging with positron emission tomography (PET). DAT occupancy was determined by displacement of 8-(2-[(18)F]fluroethyl)2beta-carbomethoxy-3beta-(4-chlorophenyl)nortropane (FECNT). DAT occupancy was between 66 and 82% and <10-41% for doses of dimethocaine and procaine that maintained maximum response rates, respectively. Acute administration of dimethocaine (10-40 mg/kg, IP) significantly increased locomotor activity and time spent on the drug-paired side and reduced the relative number of entries and time spent on the open arms of the plus-maze in mice.
1. Different local anesthetics were tested for analgesic activity in three antinociceptive models, the acetic acid-induced abdominal constriction, tail-flick and hot plate tests in the mouse. 2. In the abdominal constriction test, subcutaneous, SC, injection of lidocaine (10, 20 or 30 mg/kg) and dimethocaine (5, 10 or 20 mg/kg) induced dose-dependent antinociceptive responses. Procaine (20, 30 or 50 mg/kg) was also able to reduce the response to noxious chemical stimuli. 3. The IP injection of lidocaine and dimethocaine significantly inhibited the tail-flick and paw-licking hot plate responses; procaine was weak or inactive in these tests, in which heat was the noxious stimulus. 4. Taken together, these results suggest that antinociception produced by systemically administered lidocaine and dimethocaine at nontoxic doses in mice is due, at least in part, to their central effects.
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