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Selective GABA transporter inhibitors tiagabine and EF1502 exhibit mechanistic differences in their ability to modulate the ataxia and anticonvulsant action of the extrasynaptic GABA(A) receptor agonist gaboxadol.
Madsen KK, Ebert B, Clausen RP, Krogsgaard-Larsen P, Schousboe A, White HS. Madsen KK, et al. Among authors: clausen rp. J Pharmacol Exp Ther. 2011 Jul;338(1):214-9. doi: 10.1124/jpet.111.179671. Epub 2011 Mar 30. J Pharmacol Exp Ther. 2011. PMID: 21450931 Free PMC article.
A stereochemical anomaly: the cyclised (R)-AMPA analogue (R)-3-hydroxy-4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridine-5-carboxylic acid [(R)-5-HPCA] resembles (S)-AMPA at glutamate receptors.
Vogensen SB, Greenwood JR, Varming AR, Brehm L, Pickering DS, Nielsen B, Liljefors T, Clausen RP, Johansen TN, Krogsgaard-Larsen P. Vogensen SB, et al. Among authors: clausen rp. Org Biomol Chem. 2004 Jan 21;2(2):206-13. doi: 10.1039/b310450h. Epub 2003 Nov 24. Org Biomol Chem. 2004. PMID: 14737644
First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2.
White HS, Watson WP, Hansen SL, Slough S, Perregaard J, Sarup A, Bolvig T, Petersen G, Larsson OM, Clausen RP, Frølund B, Falch E, Krogsgaard-Larsen P, Schousboe A. White HS, et al. Among authors: clausen rp. J Pharmacol Exp Ther. 2005 Feb;312(2):866-74. doi: 10.1124/jpet.104.068825. Epub 2004 Nov 18. J Pharmacol Exp Ther. 2005. PMID: 15550575
Structure-activity relationships of selective GABA uptake inhibitors.
Høg S, Greenwood JR, Madsen KB, Larsson OM, Frølund B, Schousboe A, Krogsgaard-Larsen P, Clausen RP. Høg S, et al. Among authors: clausen rp. Curr Top Med Chem. 2006;6(17):1861-82. doi: 10.2174/156802606778249801. Curr Top Med Chem. 2006. PMID: 17017962 Review.
93 results