Naslov
Dihydroergosine: anticonflict effect in rats and enhancing effects on 3H-muscimol binding in the human brain post mortem
(Dihydroergosine: anticonflict effect in rats and enhancing effects on [3H]-muscimol binding in the human brain post mortem)

Autori
Peričić, Danka ; Tvrdeić, Ante

Izvornik
European journal of pharmacology (0014-2999) 235 (1993), 2-3; 267-274

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
dihydroergosine ; anticonflict activity ; rats ; 3H-muscimol binding ; human brain

Sažetak
The anticonflict activity of the ergot alkaloid, dihydroergosine, a drug which binds to 5-hydroxytryptamine1 (5-HT1) receptors and to gamma-aminobutyric acidA (GABAA) receptor-associated Cl- ionophore, was studied in water-deprived rats. In vitro effects of this drug on [3H]muscimol and [3H]flunitrazepam binding to the crude synaptosomal pellet of the human frontal cortex post-mortem were also investigated. Dihydroergosine, given 2 h prior to testing, enhanced drinking under punished (0.8 mA) conditions, and diminished it under unpunished conditions. The mechanism of this effect was (-)-propranolol- and pindolol-insensitive and picrotoxin-sensitive. Flumazenil either failed to affect, or at a higher dose (10 mg/kg), counteracted the dihydroergosine-induced enhancement of punished drinking. This dose of flumazenil was itself anxiogenic. Dihydroergosine had mild sedative and analgesic properties. Low concentrations of dihydroergosine (10 nM to 100 microM) enhanced the binding of [3H]muscimol but not of [3H]flunitrazepam. The results suggest that dihydroergosine may possess anxiolytic properties presumably mediated by its specific action at the GABA/benzodiazepine/chloride channel complex.

Izvorni jezik
Engleski

Znanstvena područja
Temeljne medicinske znanosti

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