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Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analogs.
Krall J, Jensen CH, Bavo F, Falk-Petersen CB, Haugaard AS, Vogensen SB, Tian Y, Nittegaard-Nielsen M, Sigurdardóttir SB, Kehler J, Kongstad KT, Gloriam DE, Clausen RP, Harpsøe K, Wellendorph P, Frølund B. Krall J, et al. Among authors: wellendorph p. J Med Chem. 2017 Nov 9;60(21):9022-9039. doi: 10.1021/acs.jmedchem.7b01351. Epub 2017 Oct 30. J Med Chem. 2017. PMID: 29028338
Design, synthesis, and in vitro pharmacology of new radiolabeled gamma-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity gamma-hydroxybutyric acid binding sites.
Sabbatini P, Wellendorph P, Høg S, Pedersen MH, Bräuner-Osborne H, Martiny L, Frølund B, Clausen RP. Sabbatini P, et al. Among authors: wellendorph p. J Med Chem. 2010 Sep 9;53(17):6506-10. doi: 10.1021/jm1006325. J Med Chem. 2010. PMID: 20715819
Chemogenomic discovery of allosteric antagonists at the GPRC6A receptor.
Gloriam DE, Wellendorph P, Johansen LD, Thomsen AR, Phonekeo K, Pedersen DS, Bräuner-Osborne H. Gloriam DE, et al. Among authors: wellendorph p. Chem Biol. 2011 Nov 23;18(11):1489-98. doi: 10.1016/j.chembiol.2011.09.012. Chem Biol. 2011. PMID: 22118683
(1S, 3S)-3-amino-4-difluoromethylenyl-1-cyclopentanoic acid (CPP-115), a potent γ-aminobutyric acid aminotransferase inactivator for the treatment of cocaine addiction.
Pan Y, Gerasimov MR, Kvist T, Wellendorph P, Madsen KK, Pera E, Lee H, Schousboe A, Chebib M, Bräuner-Osborne H, Craft CM, Brodie JD, Schiffer WK, Dewey SL, Miller SR, Silverman RB. Pan Y, et al. Among authors: wellendorph p. J Med Chem. 2012 Jan 12;55(1):357-66. doi: 10.1021/jm201231w. Epub 2011 Dec 30. J Med Chem. 2012. PMID: 22128851 Free PMC article.
α4βδ GABA(A) receptors are high-affinity targets for γ-hydroxybutyric acid (GHB).
Absalom N, Eghorn LF, Villumsen IS, Karim N, Bay T, Olsen JV, Knudsen GM, Bräuner-Osborne H, Frølund B, Clausen RP, Chebib M, Wellendorph P. Absalom N, et al. Among authors: wellendorph p. Proc Natl Acad Sci U S A. 2012 Aug 14;109(33):13404-9. doi: 10.1073/pnas.1204376109. Epub 2012 Jul 2. Proc Natl Acad Sci U S A. 2012. PMID: 22753476 Free PMC article.
Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties.
Jensen AA, Plath N, Pedersen MH, Isberg V, Krall J, Wellendorph P, Stensbøl TB, Gloriam DE, Krogsgaard-Larsen P, Frølund B. Jensen AA, et al. Among authors: wellendorph p. J Med Chem. 2013 Feb 14;56(3):1211-27. doi: 10.1021/jm301656h. Epub 2013 Jan 17. J Med Chem. 2013. PMID: 23301527
95 results