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1 Wiadomości Chemiczne

1 2004

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Ligandy receptorów gabaergicznych : struktura, właściwości, możliwość zastosowania w terapii

Malawska B., Więckowski K.

Wiadomości Chemiczne

2004

[Z] 58, 7-8

571--598

This review attempts to briefly summarize the recent development in the study of ?-aminobutyric (GABA) receptors, and their ligands. The search on compounds with agonistic and antagonistic properties of GABA receptors, the structure activity relationships, and therapeutic prospects of GABA receptors ligands was also described. GABA is the major inhibitory neurotransmitter in the brain [1-6], and influences neurons via a large number of receptor subtypes which are grouped on the basis of their pharmacology under three major classes of receptors: GABAA, GABAB, and GABAC. GABAA and GABAC receptors are ligand gated ion channels, while GABAB receptors are G-protein coupled receptors [7-10]. These receptors, especially GABAA receptors, are involved in neurological and psychiatric disorders, and are therapeutic targets in certain diseases. Several different binding sites on GABAA receptors were proposed, these include agonist sites [11-14], which also recognize competitive antagonists [15], and many positive or negative modulators sites [16-20]. GABAA receptors are modulated by benzodiazepines [21-26], barbiturates, neurosteroides [27], klomethiazol [28, 29], anesthetics [30-33], ethanol [34], some insecticides [35], furosemide [36], Zn2+ iones [37], and sites for other compounds [38-40]. Some ligands of GABAB and GABAC receptors are also presented [41-44].