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VMAT2 Inhibitors and the Path to Ingrezza (Valbenazine). Prog Med Chem. 2018; 57(1):87-111.
Harriott ND, Williams JP, Smith EB, Bozigian HP, Grigoriadis DE. PMID: 29680151.
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5 Fields:
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HumansAnimalsCells
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Differences in Dihydrotetrabenazine Isomer Concentrations Following Administration of Tetrabenazine and Valbenazine. Drugs R D. 2017 Sep; 17(3):449-459.
Skor H, Smith EB, Loewen G, O'Brien CF, Grigoriadis DE, Bozigian H. PMID: 28776237; PMCID: PMC5629142.
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3 Fields:
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HumansCells
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Single Dose and Repeat Once-Daily Dose Safety, Tolerability and Pharmacokinetics of Valbenazine in Healthy Male Subjects. Psychopharmacol Bull. 2017 08 01; 47(3):44-52.
Luo R, Bozigian H, Jimenez R, Loewen G, O'Brien CF. PMID: 28839339; PMCID: PMC5546550.
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7 Fields:
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Humans
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Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites. J Pharmacol Exp Ther. 2017 06; 361(3):454-461.
Grigoriadis DE, Smith E, Hoare SRJ, Madan A, Bozigian H. PMID: 28404690.
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20 Fields:
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A pharmacokinetic evaluation of five H(1) antagonists after an oral and intravenous microdose to human subjects. Br J Clin Pharmacol. 2009 Mar; 67(3):288-98.
Madan A, O'Brien Z, Wen J, O'Brien C, Farber RH, Beaton G, Crowe P, Oosterhuis B, Garner RC, Lappin G, Bozigian HP. PMID: 19523012; PMCID: PMC2675039.
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14 Fields:
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HumansCTClinical Trials
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Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor. J Med Chem. 2008 Dec 11; 51(23):7478-85.
Chen C, Wu D, Guo Z, Xie Q, Reinhart GJ, Madan A, Wen J, Chen T, Huang CQ, Chen M, Chen Y, Tucci FC, Rowbottom M, Pontillo J, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. PMID: 19006286.
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25 Fields:
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HumansAnimalsCells
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Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix. J Clin Endocrinol Metab. 2009 Feb; 94(2):545-51.
Struthers RS, Nicholls AJ, Grundy J, Chen T, Jimenez R, Yen SS, Bozigian HP. PMID: 19033369; PMCID: PMC2646513.
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33 Fields:
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HumansCellsCTClinical Trials
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Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity. Bioorg Med Chem Lett. 2008 Jun 01; 18(11):3301-5.
Chen C, Chen Y, Pontillo J, Guo Z, Huang CQ, Wu D, Madan A, Chen T, Wen J, Xie Q, Tucci FC, Rowbottom M, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS. PMID: 18442910.
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4 Fields:
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HumansAnimalsCells
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Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists. Bioorg Med Chem. 2008 May 15; 16(10):5606-18.
Chen C, Tucci FC, Jiang W, Tran JA, Fleck BA, Hoare SR, Wen J, Chen T, Johns M, Markison S, Foster AC, Marinkovic D, Chen CW, Arellano M, Harman J, Saunders J, Bozigian H, Marks D. PMID: 18417348.
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12 Fields:
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HumansAnimalsCells
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Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor. J Med Chem. 2007 Dec 13; 50(25):6356-66.
Tran JA, Jiang W, Tucci FC, Fleck BA, Wen J, Sai Y, Madan A, Chen TK, Markison S, Foster AC, Hoare SR, Marks D, Harman J, Chen CW, Arellano M, Marinkovic D, Bozigian H, Saunders J, Chen C. PMID: 17994683.
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4 Fields:
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HumansAnimalsCells
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In vitro metabolism of indiplon and an assessment of its drug interaction potential. Xenobiotica. 2007 Jul; 37(7):736-52.
Madan A, Fisher A, Jin L, Chapman D, Bozigian HP. PMID: 17620220.
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3 Fields:
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HumansCells
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Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. Endocrinology. 2007 Feb; 148(2):857-67.
Struthers RS, Xie Q, Sullivan SK, Reinhart GJ, Kohout TA, Zhu YF, Chen C, Liu XJ, Ling N, Yang W, Maki RA, Bonneville AK, Chen TK, Bozigian HP. PMID: 17095587.
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10 Fields:
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HumansAnimalsCells
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Suppression of serum luteinizing hormone in postmenopausal women by an orally administered nonpeptide antagonist of the gonadotropin-releasing hormone receptor (NBI-42902). J Clin Endocrinol Metab. 2006 Oct; 91(10):3903-7.
Struthers RS, Chen T, Campbell B, Jimenez R, Pan H, Yen SS, Bozigian HP. PMID: 16849403.
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10 Fields:
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HumansCTClinical Trials
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Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core. J Med Chem. 2005 Jun 16; 48(12):4100-10.
Dyck B, Grigoriadis DE, Gross RS, Guo Z, Haddach M, Marinkovic D, McCarthy JR, Moorjani M, Regan CF, Saunders J, Schwaebe MK, Szabo T, Williams JP, Zhang X, Bozigian H, Chen TK. PMID: 15943483.
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5 Fields:
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Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists. J Med Chem. 2005 Mar 10; 48(5):1540-9.
Lowe RF, Nelson J, Dang TN, Crowe PD, Pahuja A, McCarthy JR, Grigoriadis DE, Conlon P, Saunders J, Chen C, Szabo T, Chen TK, Bozigian H. PMID: 15743196.
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5 Fields:
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3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization. J Med Chem. 2005 Feb 24; 48(4):1169-78.
Tucci FC, Zhu YF, Struthers RS, Guo Z, Gross TD, Rowbottom MW, Acevedo O, Gao Y, Saunders J, Xie Q, Reinhart GJ, Liu XJ, Ling N, Bonneville AK, Chen T, Bozigian H, Chen C. PMID: 15715483.
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6 Fields:
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HumansAnimalsCells
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A novel on-line solid-phase extraction approach integrated with a monolithic column and tandem mass spectrometry for direct plasma analysis of multiple drugs and metabolites. Rapid Commun Mass Spectrom. 2005; 19(22):3259-68.
Zang X, Luo R, Song N, Chen TK, Bozigian H. PMID: 16220526.
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1 Fields:
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Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists. J Med Chem. 2004 Sep 09; 47(19):4787-98.
Chen C, Wilcoxen KM, Huang CQ, Xie YF, McCarthy JR, Webb TR, Zhu YF, Saunders J, Liu XJ, Chen TK, Bozigian H, Grigoriadis DE. PMID: 15341493.
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33 Fields:
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In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. J Pharmacol Exp Ther. 2004 Nov; 311(2):547-59.
Foster AC, Pelleymounter MA, Cullen MJ, Lewis D, Joppa M, Chen TK, Bozigian HP, Gross RS, Gogas KR. PMID: 15256538.
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5 Fields:
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Animals
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3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor. J Med Chem. 2004 Jul 01; 47(14):3483-6.
Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ, Gao Y, Rowbottom MW, Struthers RS, Reinhart GJ, Xie Q, Chen TK, Bozigian H, Killam Bonneville AL, Fisher A, Jin L, Saunders J, Chen C. PMID: 15214774.
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2 Fields:
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HumansAnimals
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Neuroprotective effects of the CRF1 antagonist R121920 after permanent focal ischemia in the rat. J Cereb Blood Flow Metab. 2001 Oct; 21(10):1208-14.
Mackay KB, Bozigian H, Grigoriadis DE, Loddick SA, Verge G, Foster AC. PMID: 11598498.
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5 Fields:
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Animals
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Comparison of the pharmacokinetics of an ondansetron solution (8 mg) when administered intravenously, orally, to the colon, and to the rectum. Pharm Res. 1994 Jan; 11(1):156-9.
Hsyu PH, Pritchard JF, Bozigian HP, Lloyd TL, Griffin RH, Shamburek R, Krishna G, Barr WH. PMID: 8140047.
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PubMed Mentions:
6 Fields:
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HumansCTClinical Trials