3-Chloro,4-methoxyfendiline is a potent GABAB receptor potentiator in rat neocortical slices
| dc.contributor.author | Ong, J. | |
| dc.contributor.author | Parker, D. | |
| dc.contributor.author | Marino, V. | |
| dc.contributor.author | Kerr, D. | |
| dc.contributor.author | Puspawati, N. | |
| dc.contributor.author | Prager, R. | |
| dc.date.issued | 2005 | |
| dc.description.abstract | Using grease-gap recording from rat neocortical slices, the GABA(B) receptor agonist baclofen elicited reversible and concentration-dependent hyperpolarizing responses (EC50=18+/-2.3 microM). The hyperpolarizations were antagonised by the GABA(B) receptor antagonist Sch 50911 [(+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid). (+)-N-1-(3-chloro-4-methoxyphenyl)ethyl-3,3-diphenylpropylamine (3-chloro,4-methoxyfendiline; 3-Cl,4-MeO-fendiline) reversibly potentiated baclofen-induced hyperpolarizing responses, which were reduced by Sch 50911, producing leftward shifts of the baclofen concentration-response curves, with a marked increase in the maximal hyperpolarization (EC50=2+/-0.5 microM). In slices preincubated with either [3H]GABA or [3H]glutamic acid, 3-Cl,4-MeO-fendiline (1 microM) potentiated the inhibitory effect of baclofen (2 microM) on the electrically evoked release of [3H]GABA and had a similar effect on the release of [3H]glutamic acid at a concentration of 0.5 microM, without affecting the basal release. These effects were blocked by Sch 50911 (10 microM). Our findings suggest that 3-Cl,4-MeO-fendiline is a potent potentiator of pre- and postsynaptic GABA(B) receptor-mediated functions. | |
| dc.identifier.citation | European Journal of Pharmacology, 2005; 507(1-3):35-42 | |
| dc.identifier.doi | 10.1016/j.ejphar.2004.11.029 | |
| dc.identifier.issn | 0014-2999 | |
| dc.identifier.issn | 1879-0712 | |
| dc.identifier.orcid | Ong, J. [0000-0002-0958-460X] | |
| dc.identifier.uri | http://hdl.handle.net/2440/16795 | |
| dc.language.iso | en | |
| dc.publisher | Elsevier Science BV | |
| dc.source.uri | https://doi.org/10.1016/j.ejphar.2004.11.029 | |
| dc.subject | Neocortex | |
| dc.subject | Baclofen | |
| dc.subject | 3-Chloro,4-methoxyfendiline | |
| dc.subject | Pre- and postsynaptic GABAB receptor | |
| dc.subject | (Rat) | |
| dc.title | 3-Chloro,4-methoxyfendiline is a potent GABAB receptor potentiator in rat neocortical slices | |
| dc.type | Journal article | |
| pubs.publication-status | Published |