Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/5996
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Type: Journal article
Title: Characterisation of GABAB ligands in vivo
Author: Humeniuk, R.
Ong, J.
Kerr, D.
White, J.
Citation: General Pharmacology, 1995; 26(2):417-424
Publisher: Pergamon
Issue Date: 1995
ISSN: 0306-3623
Statement of
Responsibility: 
Rachel E. Humeniuk, Jennifer Ong, David I.B. Kerr and Jason M. White
Abstract: 1. While GABAB antagonists have been examined in vitro, very few have been tested in vivo. A range of GABAB antagonists were tested against baclofen-induced muscle relaxation and hypothermia. 2. The GABAB antagonists exhibited a range of in vivo activity profiles. 3. CGP 35348 showed clear antagonist effects, while BPBA and 4-ABPA appeared to have agonist properties. 4. Phaclofen, 2-hydroxysaclofen, 3-APPA and 9G seemed to have little effect in this system at the doses tested. 5. Differences between in vivo and in vitro activity could be explained by differences in blood-brain barrier permeability, or possible differences in affinities for the sub-classes of GABAB receptors.
Keywords: GABAB receptor; phaclofen; 2-hydroxysaclofen; CEP 35348; BPBA; 4-ABPA; 3-APPA; 9G
Rights: Copyright © 2009 Elsevier B.V.
RMID: 0030006075
DOI: 10.1016/0306-3623(94)00175-M
Appears in Collections:Anaesthesia and Intensive Care publications

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