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Pharmacological identification of a guanidine-containing β-alanine analogue with low micromolar potency and selectivity for the betaine/GABA transporter 1 (BGT1).
Al-Khawaja A, Petersen JG, Damgaard M, Jensen MH, Vogensen SB, Lie ME, Kragholm B, Bräuner-Osborne H, Clausen RP, Frølund B, Wellendorph P. Al-Khawaja A, et al. Among authors: clausen rp. Neurochem Res. 2014 Oct;39(10):1988-96. doi: 10.1007/s11064-014-1336-9. Epub 2014 May 23. Neurochem Res. 2014. PMID: 24852577
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
94 results