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Page 1
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Dzierba CD, Bi Y, Dasgupta B, Hartz RA, Ahuja V, Cianchetta G, Kumi G, Dong L, Aleem S, Fink C, Garcia Y, Green M, Han J, Kwon S, Qiao Y, Wang J, Zhang Y, Liu Y, Zipp G, Liang Z, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Grace J, Wilson A, Nouraldeen A, Westphal R, Kimball D, Carson K, Bronson JJ, Macor JE. Dzierba CD, et al. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28. Bioorg Med Chem Lett. 2015. PMID: 25690789
Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Degnan AP, Maxwell D, Balakrishnan A, Brown JM, Easton A, Gulianello M, Hanumegowda U, Hill-Drzewi M, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Westphal R, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE. Degnan AP, et al. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5871-5876. doi: 10.1016/j.bmcl.2016.11.014. Epub 2016 Nov 9. Bioorg Med Chem Lett. 2016. PMID: 27856084
The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Bi Y, Dzierba CD, Fink C, Garcia Y, Green M, Han J, Kwon S, Kumi G, Liang Z, Liu Y, Qiao Y, Zhang Y, Zipp G, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Westphal RS, Kimball D, Bronson JJ, Macor JE. Bi Y, et al. Among authors: westphal rs. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1443-7. doi: 10.1016/j.bmcl.2015.02.038. Epub 2015 Feb 21. Bioorg Med Chem Lett. 2015. PMID: 25754495
Discovery of D1 Dopamine Receptor Positive Allosteric Modulators: Characterization of Pharmacology and Identification of Residues that Regulate Species Selectivity.
Lewis MA, Hunihan L, Watson J, Gentles RG, Hu S, Huang Y, Bronson J, Macor JE, Beno BR, Ferrante M, Hendricson A, Knox RJ, Molski TF, Kong Y, Cvijic ME, Rockwell KL, Weed MR, Cacace AM, Westphal RS, Alt A, Brown JM. Lewis MA, et al. Among authors: westphal rs. J Pharmacol Exp Ther. 2015 Sep;354(3):340-9. doi: 10.1124/jpet.115.224071. Epub 2015 Jun 24. J Pharmacol Exp Ther. 2015. PMID: 26109678
Evidence for Classical Cholinergic Toxicity Associated with Selective Activation of M1 Muscarinic Receptors.
Alt A, Pendri A, Bertekap RL Jr, Li G, Benitex Y, Nophsker M, Rockwell KL, Burford NT, Sum CS, Chen J, Herbst JJ, Ferrante M, Hendricson A, Cvijic ME, Westphal RS, O'Connell J, Banks M, Zhang L, Gentles RG, Jenkins S, Loy J, Macor JE. Alt A, et al. Among authors: westphal rs. J Pharmacol Exp Ther. 2016 Feb;356(2):293-304. doi: 10.1124/jpet.115.226910. Epub 2015 Nov 18. J Pharmacol Exp Ther. 2016. PMID: 26582730
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.
Yang F, Snyder LB, Balakrishnan A, Brown JM, Sivarao DV, Easton A, Fernandes A, Gulianello M, Hanumegowda UM, Huang H, Huang Y, Jones KM, Li YW, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Simutis FJ, Westphal R, Whiterock VJ, Bronson JJ, Macor JE, Degnan AP. Yang F, et al. ACS Med Chem Lett. 2016 Jan 4;7(3):289-93. doi: 10.1021/acsmedchemlett.5b00450. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985317 Free PMC article.
49 results