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TPA023 [7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an agonist selective for alpha2- and alpha3-containing GABAA receptors, is a nonsedating anxiolytic in rodents and primates.
Atack JR, Wafford KA, Tye SJ, Cook SM, Sohal B, Pike A, Sur C, Melillo D, Bristow L, Bromidge F, Ragan I, Kerby J, Street L, Carling R, Castro JL, Whiting P, Dawson GR, McKernan RM. Atack JR, et al. Among authors: bristow l. J Pharmacol Exp Ther. 2006 Jan;316(1):410-22. doi: 10.1124/jpet.105.089920. Epub 2005 Sep 23. J Pharmacol Exp Ther. 2006. PMID: 16183706
Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF. Kostich W, et al. Among authors: bristow l. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13. J Pharmacol Exp Ther. 2016. PMID: 27411717 Free PMC article.
Biological profile of L-745,870, a selective antagonist with high affinity for the dopamine D4 receptor.
Patel S, Freedman S, Chapman KL, Emms F, Fletcher AE, Knowles M, Marwood R, Mcallister G, Myers J, Curtis N, Kulagowski JJ, Leeson PD, Ridgill M, Graham M, Matheson S, Rathbone D, Watt AP, Bristow LJ, Rupniak NM, Baskin E, Lynch JJ, Ragan CI. Patel S, et al. Among authors: bristow lj. J Pharmacol Exp Ther. 1997 Nov;283(2):636-47. J Pharmacol Exp Ther. 1997. PMID: 9353380
Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.
Bristow LJ, Gulia J, Weed MR, Srikumar BN, Li YW, Graef JD, Naidu PS, Sanmathi C, Aher J, Bastia T, Paschapur M, Kalidindi N, Kumar KV, Molski T, Pieschl R, Fernandes A, Brown JM, Sivarao DV, Newberry K, Bookbinder M, Polino J, Keavy D, Newton A, Shields E, Simmermacher J, Kempson J, Li J, Zhang H, Mathur A, Kallem RR, Sinha M, Ramarao M, Vikramadithyan RK, Thangathirupathy S, Warrier J, Islam I, Bronson JJ, Olson RE, Macor JE, Albright CF, King D, Thompson LA, Marcin LR, Sinz M. Bristow LJ, et al. J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. doi: 10.1124/jpet.117.242784. Epub 2017 Sep 27. J Pharmacol Exp Ther. 2017. PMID: 28954811
181 results