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Items: 32

1.

VMAT2 Inhibitors and the Path to Ingrezza (Valbenazine).

Harriott ND, Williams JP, Smith EB, Bozigian HP, Grigoriadis DE.

Prog Med Chem. 2018;57(1):87-111. doi: 10.1016/bs.pmch.2017.12.002. Epub 2018 Mar 7.

PMID:
29680151
2.

Single Dose and Repeat Once-Daily Dose Safety, Tolerability and Pharmacokinetics of Valbenazine in Healthy Male Subjects.

Luo R, Bozigian H, Jimenez R, Loewen G, O'Brien CF.

Psychopharmacol Bull. 2017 Aug 1;47(3):44-52.

3.

Differences in Dihydrotetrabenazine Isomer Concentrations Following Administration of Tetrabenazine and Valbenazine.

Skor H, Smith EB, Loewen G, O'Brien CF, Grigoriadis DE, Bozigian H.

Drugs R D. 2017 Sep;17(3):449-459. doi: 10.1007/s40268-017-0202-z.

4.

Pharmacologic Characterization of Valbenazine (NBI-98854) and Its Metabolites.

Grigoriadis DE, Smith E, Hoare SRJ, Madan A, Bozigian H.

J Pharmacol Exp Ther. 2017 Jun;361(3):454-461. doi: 10.1124/jpet.116.239160. Epub 2017 Apr 12.

5.

A pharmacokinetic evaluation of five H(1) antagonists after an oral and intravenous microdose to human subjects.

Madan A, O'Brien Z, Wen J, O'Brien C, Farber RH, Beaton G, Crowe P, Oosterhuis B, Garner RC, Lappin G, Bozigian HP.

Br J Clin Pharmacol. 2009 Mar;67(3):288-98. doi: 10.1111/j.1365-2125.2008.03351.x.

6.

Suppression of gonadotropins and estradiol in premenopausal women by oral administration of the nonpeptide gonadotropin-releasing hormone antagonist elagolix.

Struthers RS, Nicholls AJ, Grundy J, Chen T, Jimenez R, Yen SS, Bozigian HP.

J Clin Endocrinol Metab. 2009 Feb;94(2):545-51. doi: 10.1210/jc.2008-1695. Epub 2008 Nov 25.

7.

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.

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.

J Med Chem. 2008 Dec 11;51(23):7478-85. doi: 10.1021/jm8006454.

PMID:
19006286
8.

Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.

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.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3301-5. doi: 10.1016/j.bmcl.2008.04.036. Epub 2008 Apr 26.

PMID:
18442910
9.

Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.

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.

Bioorg Med Chem. 2008 May 15;16(10):5606-18. doi: 10.1016/j.bmc.2008.03.072. Epub 2008 Apr 1.

PMID:
18417348
10.

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.

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.

J Med Chem. 2007 Dec 13;50(25):6356-66. Epub 2007 Nov 10.

PMID:
17994683
11.

In vitro metabolism of indiplon and an assessment of its drug interaction potential.

Madan A, Fisher A, Jin L, Chapman D, Bozigian HP.

Xenobiotica. 2007 Jul;37(7):736-52.

PMID:
17620220
12.

Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.

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.

Endocrinology. 2007 Feb;148(2):857-67. Epub 2006 Nov 9.

PMID:
17095587
13.

Suppression of serum luteinizing hormone in postmenopausal women by an orally administered nonpeptide antagonist of the gonadotropin-releasing hormone receptor (NBI-42902).

Struthers RS, Chen T, Campbell B, Jimenez R, Pan H, Yen SS, Bozigian HP.

J Clin Endocrinol Metab. 2006 Oct;91(10):3903-7. Epub 2006 Jul 18.

PMID:
16849403
14.
15.

Potent, orally active corticotropin-releasing factor receptor-1 antagonists containing a tricyclic pyrrolopyridine or pyrazolopyridine core.

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.

J Med Chem. 2005 Jun 16;48(12):4100-10.

PMID:
15943483
16.

Rational design, synthesis, and structure-activity relationships of aryltriazoles as novel corticotropin-releasing factor-1 receptor antagonists.

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.

J Med Chem. 2005 Mar 10;48(5):1540-9.

PMID:
15743196
17.

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.

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.

J Med Chem. 2005 Feb 24;48(4):1169-78.

PMID:
15715483
18.

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.

Chen C, Wilcoxen KM, Huang CQ, Xie YF, McCarthy JR, Webb TR, Zhu YF, Saunders J, Liu XJ, Chen TK, Bozigian H, Grigoriadis DE.

J Med Chem. 2004 Sep 9;47(19):4787-98.

PMID:
15341493
19.

In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic.

Foster AC, Pelleymounter MA, Cullen MJ, Lewis D, Joppa M, Chen TK, Bozigian HP, Gross RS, Gogas KR.

J Pharmacol Exp Ther. 2004 Nov;311(2):547-59. Epub 2004 Jul 15.

20.

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.

Tucci FC, Zhu YF, Guo Z, Gross TD, Connors PJ Jr, 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.

J Med Chem. 2004 Jul 1;47(14):3483-6.

PMID:
15214774
21.

Neuroprotective effects of the CRF1 antagonist R121920 after permanent focal ischemia in the rat.

Mackay KB, Bozigian H, Grigoriadis DE, Loddick SA, Verge G, Foster AC.

J Cereb Blood Flow Metab. 2001 Oct;21(10):1208-14.

PMID:
11598498
22.

Toxicity of the protein kinase C inhibitor safingol administered alone and in combination with chemotherapeutic agents.

Kedderis LB, Bozigian HP, Kleeman JM, Hall RL, Palmer TE, Harrison SD Jr, Susick RL Jr.

Fundam Appl Toxicol. 1995 May;25(2):201-17.

PMID:
7665004
23.

Ondansetron absorption in adults: effect of dosage form, food, and antacids.

Bozigian HP, Pritchard JF, Gooding AE, Pakes GE.

J Pharm Sci. 1994 Jul;83(7):1011-3.

PMID:
7965657
24.

Oral ondansetron pharmacokinetics: the effect of chemotherapy.

Hsyu PH, Pritchard JF, Bozigian HP, Gooding AE, Griffin RH, Mitchell R, Bjurstrom T, Panella TL, Huang AT, Hansen LA.

J Clin Pharmacol. 1994 Jul;34(7):767-73.

PMID:
7929872
25.

SPC-100270, a protein kinase C inhibitor, reduced hypoxic injury due to reperfusion following orthotopic liver transplantation in the rat.

Thurman RG, Gao W, Connor HD, Mason RP, Lemasters JJ, Bozigian H, Adams LM.

Transpl Int. 1994;7 Suppl 1:S167-70.

PMID:
11271195
26.

Comparison of the pharmacokinetics of an ondansetron solution (8 mg) when administered intravenously, orally, to the colon, and to the rectum.

Hsyu PH, Pritchard JF, Bozigian HP, Lloyd TL, Griffin RH, Shamburek R, Krishna G, Barr WH.

Pharm Res. 1994 Jan;11(1):156-9.

PMID:
8140047
28.

Pharmacokinetics of ranitidine in morbidly obese women.

Davis RL, Quenzer RW, Bozigian HP, Warner CW.

DICP. 1990 Nov;24(11):1040-3.

PMID:
2275223
29.

Distribution, excretion, and metabolism of butylbenzyl phthalate in the rat.

Eigenberg DA, Bozigian HP, Carter DE, Sipes IG.

J Toxicol Environ Health. 1986;17(4):445-56.

PMID:
3959124
30.

Factors influencing circadian rhythms in acetaminophen lethality.

Schnell RC, Bozigian HP, Davies MH, Merrick BA, Park KS, McMillan DA.

Pharmacology. 1984;29(3):149-57.

PMID:
6483961
31.

Circadian rhythm in acetaminophen toxicity: role of nonprotein sulfhydryls.

Schnell RC, Bozigian HP, Davies MH, Merrick BA, Johnson KL.

Toxicol Appl Pharmacol. 1983 Dec;71(3):353-61.

PMID:
6658786
32.

Circadian variations in glutathione-S-transferase and glutathione peroxidase activities in the mouse.

Davies MH, Bozigian HP, Merrick BA, Birt DF, Schnell RC.

Toxicol Lett. 1983 Oct-Nov;19(1-2):23-7.

PMID:
6658827

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