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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 90 (1986), S. 332-335 
    ISSN: 1432-2072
    Keywords: Adenosine receptor ; 3H-l-phenylisopropyladenosine binding ; 3H-N-ehtylcarboxamidoadenosine binding ; Carbamazepine ; Methylxanthine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The tricyclic anticonvulsant carbamazepine (CBZ) is effective in pain and affective disorder, but the mechanism of action for this drug has not been defined. Recently it was reported that CBZ had interaction with adenosine receptor, which is related to the inhibition of release of neurotransmitter. In the present study, we investigated the in vitro effects of CBZ and other drugs upon adenosine receptor binding using 3H-l-phenylisopropyladenosine (A1) and 3H-N-ethylcarboxamidoadenosine (A2). The following results were obtained: 1) CBZ and its derivative oxcarbazepine inhibit 3H-PIA binding at therapeutic plasma level (20–30 μM) more than they inhibit 3H-NECA binding; 2) Theophylline and caffeine, methylxanthines, which are adenosine antagonists, inhibit both bindings; 3) Other anticonvulsants such as phenobarbital, phenytoin and valproate and still other psychotropic drugs such as diazepam, imipramine and chlorpromazine have little or no effect on both bindings. These findings suggest that anticonvulsive and sedative effects of CBZ and its derivatives appear due to action on adenosine receptors (A1 and partially A2) at the therapeutic level and methylxanthines have stimulant and convulsant effects due to occupation on both A1 and A2 adenosine receptors.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1435-1463
    Keywords: Sigma receptors ; (+)-3PPP ; BMY-14802 ; in vivo microdialysis ; dopamine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Intraperitoneal injection of (+)-3-[3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3PPP), a sigma receptor agonist, significantly reduced the striatal levels of dopamine (DA), 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) measured by in vivo microdialysis. These reductions were significantly greater at (+)-3PPP doses of 12 and 24 mg/kg than at 1 mg/ kg. The levels of 5-hydroxyindoleacetic acid (5HIAA) were increased by the injection of (+)-3PPP in dose of 24 mg/kg, but were not affected at lower doses. BMY-14802, a sigma antagonist, alone at doses of 15 mg/kg and 30 mg/kg did not affect the levels of DA, DOPAC, HVA and 5HIAA. Pretreatment with 30 mg/kg BMY-14802 reversed the reduction of the levels of DA induced by 12 mg/kg (+)-3PPP. Although neither 30 mg/kg BMY-14802 nor 12 mg/kg (+)-3PPP affected the levels of striatal 5HIAA, combined treatment with both produced a significant elevation. These findings clearly demonstrate that sigma receptors may regulate DA release from the striatal presynapse.
    Type of Medium: Electronic Resource
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