The Non-Anaesthetic Propofol Analogue 2,6-Di-tert-Butylphenol Fails to Modulate GABAA Receptor Function
J Ahrens, M Leuwer, J De La Roche, N Foadi… - Pharmacology, 2009 - karger.com
J Ahrens, M Leuwer, J De La Roche, N Foadi, K Krampfl, G Haeseler
Pharmacology, 2009•karger.comModulation of inhibitory synaptic transmission within the central nervous system contributes
considerably to the anaesthetic effects of propofol and its analogues in vivo. We have
studied the effects of the non-anaesthetic propofol analogue 2, 6-di-tert-butylphenol on rat
α1β2γ2 GABAA receptors expressed in a mammalian expression system (HEK 293 cells)
using the whole-cell patch clamp technique. Our experiments showed that 2, 6-di-tert-
butylphenol completely lacks co-activation and direct activation of the inhibitory GABAA …
considerably to the anaesthetic effects of propofol and its analogues in vivo. We have
studied the effects of the non-anaesthetic propofol analogue 2, 6-di-tert-butylphenol on rat
α1β2γ2 GABAA receptors expressed in a mammalian expression system (HEK 293 cells)
using the whole-cell patch clamp technique. Our experiments showed that 2, 6-di-tert-
butylphenol completely lacks co-activation and direct activation of the inhibitory GABAA …
Abstract
Modulation of inhibitory synaptic transmission within the central nervous system contributes considerably to the anaesthetic effects of propofol and its analogues in vivo. We have studied the effects of the non-anaesthetic propofol analogue 2,6-di-tert-butylphenol on rat α1β2γ2 GABAA receptors expressed in a mammalian expression system (HEK 293 cells) using the whole-cell patch clamp technique. Our experiments showed that 2,6-di-tert-butylphenol completely lacks co-activation and direct activation of the inhibitory GABAA receptor. Our results support the assumption that modulation of inhibitory GABAA receptor function is responsible for the anaesthetic effects of propofol in vivo.
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