Academic Journal
The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors
| العنوان: | The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors |
|---|---|
| المؤلفون: | C. J. Weir, A. T. Y. Ling, D. Belelli, J. A. W. Wildsmith, J. A. Peters, J. J. Lambert |
| المساهمون: | The Pennsylvania State University CiteSeerX Archives |
| المصدر: | http://bja.oxfordjournals.org/content/92/5/704.full.pdf. |
| سنة النشر: | 2004 |
| المجموعة: | CiteSeerX |
| الوصف: | Background. Anaesthetic steroids are established positive allosteric modulators of GABAA receptors, but little is known concerning steroid modulation of strychnine-sensitive glycine receptors, the principal mediators of fast, inhibitory neurotransmission in the brain stem and spinal cord. This study compared the modulatory actions of ®ve anaesthetic pregnane steroids and two non-anaesthetic isomers at human recombinant a1 glycine and a1b2g2L GABAA recep-tors. Methods. Recombinant a1 glycine or a1b2g2L GABAA receptors were expressed in Xenopus laevis oocytes and agonist-evoked currents recorded under voltage-clamp. Steroid modulation of currents evoked by GABA, or glycine, was quanti®ed by determining the potency (EC50) and maximal effect of the compounds. Results. The anaesthetics minaxolone (EC50=1.3 mM), Org20599 (EC50=1.1 mM) and alphaxa-lone (EC50=2.2 mM) enhanced currents mediated by GABAA receptors. The anaesthetics also enhanced currents mediated by glycine receptors, although with higher EC50 values (minaxo-lone 13.1 mM; Org20599=22.9 mM and alphaxalone=27.8 mM). The maximal enhancement (to 780±950 % of control) produced by the three steroids acting at the GABAA receptor was simi- |
| نوع الوثيقة: | text |
| وصف الملف: | application/pdf |
| اللغة: | English |
| Relation: | http://citeseerx.ist.psu.edu/viewdoc/summary?doi=10.1.1.519.3591; http://bja.oxfordjournals.org/content/92/5/704.full.pdf |
| الاتاحة: | http://citeseerx.ist.psu.edu/viewdoc/summary?doi=10.1.1.519.3591 http://bja.oxfordjournals.org/content/92/5/704.full.pdf |
| Rights: | Metadata may be used without restrictions as long as the oai identifier remains attached to it. |
| رقم الانضمام: | edsbas.D4675A24 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |