Characterisation of GABAB ligands in vivo

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dc.contributor.authorHumeniuk, R.
dc.contributor.authorOng, J.
dc.contributor.authorKerr, D.
dc.contributor.authorWhite, J.
dc.date.issued1995
dc.description.abstract1. 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.
dc.description.statementofresponsibilityRachel E. Humeniuk, Jennifer Ong, David I.B. Kerr and Jason M. White
dc.identifier.citationGeneral pharmacology, 1995; 26(2):417-424
dc.identifier.doi10.1016/0306-3623(94)00175-M
dc.identifier.issn0306-3623
dc.identifier.orcidOng, J. [0000-0002-0958-460X]
dc.identifier.urihttp://hdl.handle.net/2440/5996
dc.language.isoen
dc.publisherPergamon
dc.rightsCopyright © 2009 Elsevier B.V.
dc.source.urihttps://doi.org/10.1016/0306-3623(94)00175-m
dc.subjectGABAB receptor
dc.subjectphaclofen
dc.subject2-hydroxysaclofen
dc.subjectCEP 35348
dc.subjectBPBA
dc.subject4-ABPA
dc.subject3-APPA
dc.subject9G
dc.titleCharacterisation of GABAB ligands in vivo
dc.typeJournal article
pubs.publication-statusPublished

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