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Page 1
GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.
Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Clawson DK, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Martinez-Perez JA, et al. Among authors: stack dr. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. doi: 10.1016/j.bmcl.2013.09.045. Epub 2013 Sep 24. Bioorg Med Chem Lett. 2013. PMID: 24140446
Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.
Filla SA, Winter MA, Johnson KW, Bleakman D, Bell MG, Bleisch TJ, Castaño AM, Clemens-Smith A, del Prado M, Dieckman DK, Dominguez E, Escribano A, Ho KH, Hudziak KJ, Katofiasc MA, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Phebus LA, Stack DR, Stratford RE, Ornstein PL. Filla SA, et al. Among authors: stack dr. J Med Chem. 2002 Sep 26;45(20):4383-6. doi: 10.1021/jm025548q. J Med Chem. 2002. PMID: 12238915
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
Dominguez E, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Buckmaster JL, Castano AM, Del Prado M, Escribano A, Filla SA, Ho KH, Hudziak KJ, Jones CK, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Dominguez E, et al. Among authors: stack dr. J Med Chem. 2005 Jun 30;48(13):4200-3. doi: 10.1021/jm0491952. J Med Chem. 2005. PMID: 15974569
GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models.
Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Arnold BM, Bell MG, Bleisch TJ, Castaño AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL. Martinez-Perez JA, et al. Among authors: stack dr. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6459-62. doi: 10.1016/j.bmcl.2013.09.046. Epub 2013 Sep 25. Bioorg Med Chem Lett. 2013. PMID: 24119554
Identification of LY3522348: A Highly Selective and Orally Efficacious Ketohexokinase Inhibitor.
Durham TB, Hao J, Spinazze P, Stack DR, Toth JL, Massey S, Mbofana CT, Johnston RD, Lineswala JP, Wrobleski A, Mínguez JM, Perez C, Smith DL, Lamar J, Leon R, Corkins C, Durbin J, Tung F, Guo S, Linder RJ, Yumibe N, Wang W, MacKrell J, Antonellis M, Mascaro B. Durham TB, et al. Among authors: stack dr. J Med Chem. 2023 Dec 14;66(23):15960-15976. doi: 10.1021/acs.jmedchem.3c01410. Epub 2023 Nov 22. J Med Chem. 2023. PMID: 37992274