Effect of Ergot Alkaloids on 3H-Flunitrazepam Binding to Mouse Brain GABAA ReceptorsReportar como inadecuado




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Collegium antropologicum, Vol.27 - Supplement 1 No.1 June 2003. -

In vitro effects of dihydroergotoxine, dihydroergosine, dihydroergotamine, -dihydroergocriptine

ergot alkaloids, diazepam, methyl--Carboline-3-carboxilate -CCM,

flumazenil benzodiazepines, -amino butyric acid GABA and thiopental barbiturate

were studied on mouse brain cerebrum minus cerebral cortex benzodiazepine

binding sites labeled with 3H-flunitrazepam. Specific, high affinity affinity constant,

Kd = 57.7 8.6 nM binding sites for 3H-flunitrazepam on mouse brain membranes were

identified. All benzodiazepine drugs inhibited 3H-flunitrazepam binding with nanomolar

potencies. In contrast to benzodiazepines, all ergot drugs, GABA and thiopental produced

an enhancement of 3H-flunitrazepam binding to its binding site at the GABAA receptor

of the mouse brain. The rank order of potency was: neurotransmitter GABA >

dihydroergotoxine > thiopental > -dihydroergocriptine > dihydroergosine > dihydroergotamine.

The results suggest that dihydrogenated ergot derivatives do not bind to the

brain benzodiazepine binding sites labeled with 3H-flunitrazepam. However, an enhancement

of 3H-flunitrazepam binding by all ergot drugs tested, clearly identifies an allosteric

interaction with the benzodiazepine binding sites of GABAA receptors.

ergot drugs; 3H-flunitrazepam; GABAA; mouse



Autor: Ante Tvrdeić - Danka Peričić -

Fuente: http://hrcak.srce.hr/



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