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  • Ligand binding  (1)
  • Lobeline  (1)
  • Mecamylamine Locomotor activity  (1)
  • 1
    ISSN: 1432-2072
    Keywords: Nicotine ; 1-Acetyl-4-methylpiperazine ; Mecamylamine ; DMPP ; Ligand binding ; Locomotor activity ; Drug discrimination
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The novel nicotinic agonist 1-acetyl-4-methylpiperazine (AMP) has been studied in ligand-binding and behavioural studies. AMP methiodide potently inhibited [3H]-(−)-nicotine and [125I]-α-bungarotoxin binding to P2 membranes from rat brain and [125I]-α-bungarotoxin binding to rat skeletal muscles. AMP HCl also inhibited nicotinic binding, but it was 100 times less potent than AMP methiodide. In behavioural studies, AMP HCl reduced locomotor activity of experimentally naive rats and mecamylamine blocked this effect. In rats receiving (−)-nicotine chronically, AMP HCl did not increase locomotor activity consistently or to the same extent as (−)-nicotine. In rats trained to discriminate (−)-nicotine from saline in a two-bar operant conditioning procedure with food reinforcement, there was generalization to AMP HCl, but only at doses that reduced the overall rate of responding. The potency and effectiveness of AMP relative to (−)-nicotine varied across the different behavioural procedures. The results suggest that the pharmacodynamic action of AMP differs from that of (−)-nicotine and that it usefully extends the range of agonists that can be used as probes for central nicotinic mechanisms.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 117 (1995), S. 430-437 
    ISSN: 1432-2072
    Keywords: Nicotine ; Lobeline ; Isoarecolone ; Nornicotine ; Anabasine ; Cytisine ; Mecamylamine Locomotor activity ; Rats
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects of nicotine and related compounds on locomotor activity were compared in experimentally naive rats and in animals chronically exposed to nicotine and the photocell test chambers. In experimentally naive rats, all nicotinic compounds decreased locomotion in a dose-related manner and the rank order of potency was (−)-nicotine〉(+)-nornicotine〉(+)-nicotine 〉 cytisine 〉 lobeline 〉 anabasine. Mecamylamine attenuated the locomotor depressant effects of most of the agonists, except lobeline. In rats previously exposed to nicotine and the test apparatus for several weeks, (−)-nicotine increased locomotor activity in a dose-related manner, with a maximal increase to 400% of baseline at a dose of 0.4 mg/kg. One or more doses of (+)-nicotine, (+)-nornicotine and anabasine also increased locomotor activity in these animals, although the maximal effects seen were in all cases less than the maximal effect of (−)-nicotine. Cytisine and lobeline failed to increase locomotor activity at any dose tested. These conclusions were not altered by consideration of the time-courses for the effects of the different drugs. Thus, the results confirm that the locomotor stimulant and depressant effects of nicotine can be dissociated from each other, a finding that may be explained by differences in their actions at nicotinic receptors.
    Type of Medium: Electronic Resource
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