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In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
Malysz J, Grønlien JH, Anderson DJ, Håkerud M, Thorin-Hagene K, Ween H, Wetterstrand C, Briggs CA, Faghih R, Bunnelle WH, Gopalakrishnan M. Malysz J, et al. Among authors: gopalakrishnan m. J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. doi: 10.1124/jpet.109.151886. Epub 2009 Apr 23. J Pharmacol Exp Ther. 2009. PMID: 19389923
An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo.
Timmermann DB, Grønlien JH, Kohlhaas KL, Nielsen EØ, Dam E, Jørgensen TD, Ahring PK, Peters D, Holst D, Christensen JK, Malysz J, Briggs CA, Gopalakrishnan M, Olsen GM. Timmermann DB, et al. Among authors: gopalakrishnan m. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307. doi: 10.1124/jpet.107.120436. Epub 2007 Jul 11. J Pharmacol Exp Ther. 2007. PMID: 17625074
Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways.
Bitner RS, Bunnelle WH, Anderson DJ, Briggs CA, Buccafusco J, Curzon P, Decker MW, Frost JM, Gronlien JH, Gubbins E, Li J, Malysz J, Markosyan S, Marsh K, Meyer MD, Nikkel AL, Radek RJ, Robb HM, Timmermann D, Sullivan JP, Gopalakrishnan M. Bitner RS, et al. Among authors: gopalakrishnan m. J Neurosci. 2007 Sep 26;27(39):10578-87. doi: 10.1523/JNEUROSCI.2444-07.2007. J Neurosci. 2007. PMID: 17898229 Free PMC article.
[3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain.
Anderson DJ, Bunnelle W, Surber B, Du J, Surowy C, Tribollet E, Marguerat A, Bertrand D, Gopalakrishnan M. Anderson DJ, et al. Among authors: gopalakrishnan m. J Pharmacol Exp Ther. 2008 Jan;324(1):179-87. doi: 10.1124/jpet.107.130062. Epub 2007 Oct 24. J Pharmacol Exp Ther. 2008. PMID: 17959745
Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties.
Tietje KR, Anderson DJ, Bitner RS, Blomme EA, Brackemeyer PJ, Briggs CA, Browman KE, Bury D, Curzon P, Drescher KU, Frost JM, Fryer RM, Fox GB, Gronlien JH, Håkerud M, Gubbins EJ, Halm S, Harris R, Helfrich RJ, Kohlhaas KL, Law D, Malysz J, Marsh KC, Martin RL, Meyer MD, Molesky AL, Nikkel AL, Otte S, Pan L, Puttfarcken PS, Radek RJ, Robb HM, Spies E, Thorin-Hagene K, Waring JF, Ween H, Xu H, Gopalakrishnan M, Bunnelle WH. Tietje KR, et al. Among authors: gopalakrishnan m. CNS Neurosci Ther. 2008 Spring;14(1):65-82. doi: 10.1111/j.1527-3458.2008.00037.x. CNS Neurosci Ther. 2008. PMID: 18482100 Free PMC article. Review.
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
Faghih R, Gopalakrishnan SM, Gronlien JH, Malysz J, Briggs CA, Wetterstrand C, Ween H, Curtis MP, Sarris KA, Gfesser GA, El-Kouhen R, Robb HM, Radek RJ, Marsh KC, Bunnelle WH, Gopalakrishnan M. Faghih R, et al. Among authors: gopalakrishnan sm, gopalakrishnan m. J Med Chem. 2009 May 28;52(10):3377-84. doi: 10.1021/jm9003818. J Med Chem. 2009. PMID: 19419141
Stimulation of dopamine release by nicotinic acetylcholine receptor ligands in rat brain slices correlates with the profile of high, but not low, sensitivity alpha4beta2 subunit combination.
Anderson DJ, Malysz J, Grønlien JH, El Kouhen R, Håkerud M, Wetterstrand C, Briggs CA, Gopalakrishnan M. Anderson DJ, et al. Among authors: gopalakrishnan m. Biochem Pharmacol. 2009 Oct 1;78(7):844-51. doi: 10.1016/j.bcp.2009.06.024. Epub 2009 Jun 23. Biochem Pharmacol. 2009. PMID: 19555668
459 results