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https://hdl.handle.net/2440/5991
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Type: | Journal article |
Title: | The morpholino-acetic acid analogue Sch 50911 is a selective GABAB receptor antagonist in rat neocortical slices |
Author: | Ong, J. Marino, V. Parker, D. Kerr, D. Blythin, D. |
Citation: | European Journal of Pharmacology, 1998; 362(1):35-41 |
Publisher: | ELSEVIER SCIENCE BV |
Issue Date: | 1998 |
ISSN: | 0014-2999 1879-0712 |
Statement of Responsibility: | Jennifer Ong, Victor Marino, David A.S. Parker, David I.B. Kerr, David J. Blythin |
Abstract: | The pharmacological properties of (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid (Sch 50911) were evaluated on GABA(B) receptors in rat neocortical slices. The GABA(B) receptor agonist, baclofen, produced a concentration-dependent depression of the frequency of spontaneous discharges in slices maintained in Mg2+-free Krebs medium with an EC50 of 6 microM, reversibly antagonised by Sch 50911 (5, 10 and 25 microM) with an apparent pA2 of 6.0 +/- 0.1. The (-) enantiomer Sch 50910 (500 microM) and the racemic des-methyl analogue Sch 48588 (500 microM) were inactive. In slices preloaded with [3H]GABA, Sch 50911 antagonised GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow in a concentration-dependent manner, with an IC50 of 3 microM. The maximal effect (148 +/- 10.5%) was found at 10 microM, but at 50 microM the response was reduced to 67 +/- 19%. In contrast, evoked release was unaffected by Sch 50910 (100 microM) whilst Sch 48588 at 100 microM increased the overflow by 51.3 +/- 11.6%. In summary, Sch 50911 is a relatively potent antagonist of considerable potential in studies of GABA(B) receptor function. |
Keywords: | Neocortex Animals Rats Rats, Sprague-Dawley Baclofen Morpholines GABA Antagonists Dose-Response Relationship, Drug Male GABA-B Receptor Antagonists In Vitro Techniques |
DOI: | 10.1016/S0014-2999(98)00723-7 |
Published version: | http://dx.doi.org/10.1016/s0014-2999(98)00723-7 |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 5 |
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