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State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects.
Gould RW, Nedelcovych MT, Gong X, Tsai E, Bubser M, Bridges TM, Wood MR, Duggan ME, Brandon NJ, Dunlop J, Wood MW, Ivarsson M, Noetzel MJ, Daniels JS, Niswender CM, Lindsley CW, Conn PJ, Jones CK. Gould RW, et al. Among authors: bubser m. Neuropharmacology. 2016 Mar;102:244-53. doi: 10.1016/j.neuropharm.2015.11.016. Epub 2015 Nov 23. Neuropharmacology. 2016. PMID: 26617071 Free PMC article.
Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100.
Byun NE, Grannan M, Bubser M, Barry RL, Thompson A, Rosanelli J, Gowrishankar R, Kelm ND, Damon S, Bridges TM, Melancon BJ, Tarr JC, Brogan JT, Avison MJ, Deutch AY, Wess J, Wood MR, Lindsley CW, Gore JC, Conn PJ, Jones CK. Byun NE, et al. Among authors: bubser m. Neuropsychopharmacology. 2014 Jun;39(7):1578-93. doi: 10.1038/npp.2014.2. Epub 2014 Jan 20. Neuropsychopharmacology. 2014. PMID: 24442096 Free PMC article.
Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK. Bubser M, et al. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. Epub 2014 Aug 19. ACS Chem Neurosci. 2014. PMID: 25137629 Free PMC article.
Pharmacological stimulation of metabotropic glutamate receptor type 4 in a rat model of Parkinson's disease and L-DOPA-induced dyskinesia: Comparison between a positive allosteric modulator and an orthosteric agonist.
Iderberg H, Maslava N, Thompson AD, Bubser M, Niswender CM, Hopkins CR, Lindsley CW, Conn PJ, Jones CK, Cenci MA. Iderberg H, et al. Among authors: bubser m. Neuropharmacology. 2015 Aug;95:121-9. doi: 10.1016/j.neuropharm.2015.02.023. Epub 2015 Mar 4. Neuropharmacology. 2015. PMID: 25749357 Free PMC article.
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Wood MR, et al. Among authors: bubser m. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3029-3033. doi: 10.1016/j.bmcl.2016.05.010. Epub 2016 May 5. Bioorg Med Chem Lett. 2016. PMID: 27185330 Free PMC article.
Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.
Wood MR, Noetzel MJ, Poslusney MS, Melancon BJ, Tarr JC, Lamsal A, Chang S, Luscombe VB, Weiner RL, Cho HP, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Wood MR, et al. Among authors: bubser m. Bioorg Med Chem Lett. 2017 Jan 15;27(2):171-175. doi: 10.1016/j.bmcl.2016.11.086. Epub 2016 Nov 30. Bioorg Med Chem Lett. 2017. PMID: 27939174 Free PMC article.
Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.
Melancon BJ, Wood MR, Noetzel MJ, Nance KD, Engelberg EM, Han C, Lamsal A, Chang S, Cho HP, Byers FW, Bubser M, Jones CK, Niswender CM, Wood MW, Engers DW, Wu D, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW. Melancon BJ, et al. Among authors: bubser m. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2296-2301. doi: 10.1016/j.bmcl.2017.04.043. Epub 2017 Apr 13. Bioorg Med Chem Lett. 2017. PMID: 28442253 Free PMC article.
Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154.
Gould RW, Grannan MD, Gunter BW, Ball J, Bubser M, Bridges TM, Wess J, Wood MW, Brandon NJ, Duggan ME, Niswender CM, Lindsley CW, Conn PJ, Jones CK. Gould RW, et al. Among authors: bubser m. Neuropharmacology. 2018 Jan;128:492-502. doi: 10.1016/j.neuropharm.2017.07.013. Epub 2017 Jul 17. Neuropharmacology. 2018. PMID: 28729220 Free PMC article.
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.
Yohn SE, Foster DJ, Covey DP, Moehle MS, Galbraith J, Garcia-Barrantes PM, Cho HP, Bubser M, Blobaum AL, Joffe ME, Cheer JF, Jones CK, Lindsley CW, Conn PJ. Yohn SE, et al. Among authors: bubser m. Mol Psychiatry. 2020 Nov;25(11):2786-2799. doi: 10.1038/s41380-018-0206-2. Epub 2018 Aug 16. Mol Psychiatry. 2020. PMID: 30116027 Free PMC article.
80 results