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Mutant human alpha(1)beta(1)(T262Q) GABA(A) receptors are directly activated but not modulated by pentobarbital.
John Curtin School of Medical Research, Australian National University.
1999 (English)In: European Journal of Pharmacology, ISSN 0014-2999, E-ISSN 1879-0712, Vol. 385, no 2-3, 283-6 p.Article in journal (Refereed) Published
Abstract [en]

Pentobarbital activates GABA(A) receptors and enhances GABA-activated currents. A threonine residue (262) in the second membrane spanning region at the 12' position in the beta(1) subunit, alpha(1)beta(1)(T12'Q), is necessary for the potentiating action of pentobarbital. We examined whether T12'Q-mutated receptors expressed in Spodoptera frugipedra (Sf 9) cells responded to direct activation by pentobarbital. In both mutant and wild type receptors, pentobarbital (100 microM to 1 mM) evoked a current response. The pentobarbital EC(50) values were similar; 119 and 158 microM for alpha(1)beta(1) and alpha(1)beta(1)(T12'Q) receptors, respectively. The results show it is possible to discriminate between agonistic and potentiating effects of pentobarbital, suggesting these actions involve separate mechanisms.

Place, publisher, year, edition, pages
1999. Vol. 385, no 2-3, 283-6 p.
National Category
URN: urn:nbn:se:uu:diva-182787PubMedID: 10607887OAI: oai:DiVA.org:uu-182787DiVA: diva2:560712
Available from: 2012-10-15 Created: 2012-10-15 Last updated: 2012-10-15

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