Actions of thienyl analogs of baclofen at GABAB receptors in rat neocortical slices

Date

1997

Authors

Ong, J.
Kerr, D.
Vaccher, C.
Berthelot, P.

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Journal article

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European Journal of Pharmacology, 1997; 329(2-3):133-136

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Jennifer Ong, David I.B. Kerr, Claude Vaccher, Pascal Berthelot

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Abstract

In rat neocortical slices maintained in Mg2+-free Krebs medium, baclofen and its thienyl analogs, 4-amino-3-(5-chlorothien-2-yl)-butanoic acid (5h), 4-amino-3-(5-methylthien-2-yl)-butanoic acid (5d), 4-amino-3-(5-bromothien-2-yl)-butanoic acid (5f) and 4-amino-3-(thien-3-yl)-butanoic acid (5j) dose-dependently suppressed the spontaneous discharges, antagonised by the GABA(B) receptor antagonist 2-hydroxysaclofen (200 microM). Their relative potencies were baclofen > 5h > 5d > 5f > 5j. These heterocyclic analogs may prove useful as GABA(B) receptor agonists in functional studies.

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Dissertation Note

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Short communication

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© 1997 Elsevier Science B.V.

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