UCL logo

UCL Discovery

UCL home » Library Services » Electronic resources » UCL Discovery

The kinetics of inhibition of rat recombinant heteromeric 1β glycine receptors by the low-affinity antagonist SR-95531

Beato, M.; Burzomato, V.; Sivilotti, L.G.; (2007) The kinetics of inhibition of rat recombinant heteromeric 1β glycine receptors by the low-affinity antagonist SR-95531. J PHYSIOL-LONDON , 580 (1) pp. 171-179. 10.1113/jphysiol.2006.126888.

Full text not available from this repository.

Abstract

The GABAA antagonist SR-95531 (gabazine) is known to block glycine receptors, albeit with low affinity. We have studied the effect of SR-95531 on rat recombinant {alpha}1beta glycine receptors expressed in human embryonic kidney (HEK293) cells by recording macroscopic currents elicited by rapid glycine application to outside-out patches. SR-95531 has a fast unbinding rate (koffSR, about 3000 s–1) and this means that the time course of its unbinding is comparable to the expected time course of the transmitter in the cleft. We also found that equilibrium applications of SR-95531 reduced the response to brief glycine applications by an amount inversely proportional to the duration of glycine application. The fast unbinding rate of SR-95531 from the glycine receptor will make it useful for establishing the time course of glycine concentration at glycinergic synapses.

Type: Article
Title: The kinetics of inhibition of rat recombinant heteromeric 1β glycine receptors by the low-affinity antagonist SR-95531
DOI: 10.1113/jphysiol.2006.126888
Publisher version: http://dx.doi.org/10.1113/jphysiol.2006.126888
Language: English
Keywords: GLYCINE RECEPTORS, POINT MUTATION, BINDING-SITES, STOICHIOMETRY, SUBUNIT, RESPONSES, GLUTAMATE
UCL classification: UCL > School of Life and Medical Sciences > Faculty of Life Sciences > Biosciences (Division of) > Neuroscience, Physiology and Pharmacology
URI: http://discovery.ucl.ac.uk/id/eprint/9482
Downloads since deposit
0Downloads
Download activity - last month
Download activity - last 12 months
Downloads by country - last 12 months

Archive Staff Only

View Item View Item