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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.


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.


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.


Non-peptide CRF-Receptor Antagonists: Allosterism, Kinetics and Translation to Efficacy in Human Disease.

Hoare SRJ, Grigoriadis DE.

Curr Mol Pharmacol. 2017;10(4):282-295. doi: 10.2174/1874467210666170110124539. Review.


The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not of Anti-Craving Effects.

Schwandt ML, Cortes CR, Kwako LE, George DT, Momenan R, Sinha R, Grigoriadis DE, Pich EM, Leggio L, Heilig M.

Neuropsychopharmacology. 2016 Nov;41(12):2818-2829. doi: 10.1038/npp.2016.61. Epub 2016 Apr 25.


Single-Dose Study of a Corticotropin-Releasing Factor Receptor-1 Antagonist in Women With 21-Hydroxylase Deficiency.

Turcu AF, Spencer-Segal JL, Farber RH, Luo R, Grigoriadis DE, Ramm CA, Madrigal D, Muth T, O'Brien CF, Auchus RJ.

J Clin Endocrinol Metab. 2016 Mar;101(3):1174-80. doi: 10.1210/jc.2015-3574. Epub 2016 Jan 11.


Corticotropin-releasing factor receptor subtype 2 in human colonic mucosa: down-regulation in ulcerative colitis.

Chatzaki E, Anton PA, Million M, Lambropoulou M, Constantinidis T, Kolios G, Taché Y, Grigoriadis DE.

World J Gastroenterol. 2013 Mar 7;19(9):1416-23. doi: 10.3748/wjg.v19.i9.1416.


Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.

Fleck BA, Hoare SR, Pick RR, Bradbury MJ, Grigoriadis DE.

J Pharmacol Exp Ther. 2012 May;341(2):518-31. doi: 10.1124/jpet.111.188714. Epub 2012 Feb 22.


Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties.

Tellew JE, Lanier M, Moorjani M, Lin E, Luo Z, Slee DH, Zhang X, Hoare SR, Grigoriadis DE, St Denis Y, Di Fabio R, Di Modugno E, Saunders J, Williams JP.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7259-64. doi: 10.1016/j.bmcl.2010.10.095. Epub 2010 Oct 25.


Hippocampal dysfunction and cognitive impairments provoked by chronic early-life stress involve excessive activation of CRH receptors.

Ivy AS, Rex CS, Chen Y, Dubé C, Maras PM, Grigoriadis DE, Gall CM, Lynch G, Baram TZ.

J Neurosci. 2010 Sep 29;30(39):13005-15. doi: 10.1523/JNEUROSCI.1784-10.2010.


CRF system recruitment mediates dark side of compulsive eating.

Cottone P, Sabino V, Roberto M, Bajo M, Pockros L, Frihauf JB, Fekete EM, Steardo L, Rice KC, Grigoriadis DE, Conti B, Koob GF, Zorrilla EP.

Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20016-20. doi: 10.1073/pnas.0908789106. Epub 2009 Nov 9.


Drugability of extracellular targets: discovery of small molecule drugs targeting allosteric, functional, and subunit-selective sites on GPCRs and ion channels.

Grigoriadis DE, Hoare SR, Lechner SM, Slee DH, Williams JA.

Neuropsychopharmacology. 2009 Jan;34(1):106-25. doi: 10.1038/npp.2008.149. Epub 2008 Sep 17. Review.


Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation.

Hoare SR, Fleck BA, Gross RS, Crowe PD, Williams JP, Grigoriadis DE.

Mol Pharmacol. 2008 May;73(5):1371-80. doi: 10.1124/mol.107.042978. Epub 2008 Jan 31.


High-affinity CRF1 receptor antagonist NBI-34041: preclinical and clinical data suggest safety and efficacy in attenuating elevated stress response.

Ising M, Zimmermann US, Künzel HE, Uhr M, Foster AC, Learned-Coughlin SM, Holsboer F, Grigoriadis DE.

Neuropsychopharmacology. 2007 Sep;32(9):1941-9. Epub 2007 Feb 7.


Cocaine withdrawal enhances long-term potentiation induced by corticotropin-releasing factor at central amygdala glutamatergic synapses via CRF, NMDA receptors and PKA.

Pollandt S, Liu J, Orozco-Cabal L, Grigoriadis DE, Vale WW, Gallagher JP, Shinnick-Gallagher P.

Eur J Neurosci. 2006 Sep;24(6):1733-43.


Corticotropin-releasing factor (CRF) receptor type 2 in the human stomach: protective biological role by inhibition of apoptosis.

Chatzaki E, Lambropoulou M, Constantinidis TC, Papadopoulos N, Taché Y, Minopoulos G, Grigoriadis DE.

J Cell Physiol. 2006 Dec;209(3):905-11.


Corticotropin-releasing hormone receptor 2-deficient mice have reduced intestinal inflammatory responses.

Kokkotou E, Torres D, Moss AC, O'Brien M, Grigoriadis DE, Karalis K, Pothoulakis C.

J Immunol. 2006 Sep 1;177(5):3355-61.


Cellular and molecular mechanisms of hippocampal activation by acute stress are age-dependent.

Chen Y, Fenoglio KA, Dubé CM, Grigoriadis DE, Baram TZ.

Mol Psychiatry. 2006 Nov;11(11):992-1002. Epub 2006 Jun 27.


Single amino acid residue determinants of non-peptide antagonist binding to the corticotropin-releasing factor1 (CRF1) receptor.

Hoare SR, Brown BT, Santos MA, Malany S, Betz SF, Grigoriadis DE.

Biochem Pharmacol. 2006 Jul 14;72(2):244-55. Epub 2006 Apr 25.


Impact of state of arousal and stress neuropeptides on urodynamic function in freely moving rats.

Kiddoo DA, Valentino RJ, Zderic S, Ganesh A, Leiser SC, Hale L, Grigoriadis DE.

Am J Physiol Regul Integr Comp Physiol. 2006 Jun;290(6):R1697-706. Epub 2006 Jan 26.


Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.

Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP.

J Med Chem. 2005 Sep 8;48(18):5780-93.


Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.

Guo Z, Tellew JE, Gross RS, Dyck B, Grey J, Haddach M, Kiankarimi M, Lanier M, Li BF, Luo Z, McCarthy JR, Moorjani M, Saunders J, Sullivan R, Zhang X, Zamani-Kord S, Grigoriadis DE, Crowe PD, Chen TK, Williams JP.

J Med Chem. 2005 Aug 11;48(16):5104-7.


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.


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.


Chronic cocaine administration switches corticotropin-releasing factor2 receptor-mediated depression to facilitation of glutamatergic transmission in the lateral septum.

Liu J, Yu B, Orozco-Cabal L, Grigoriadis DE, Rivier J, Vale WW, Shinnick-Gallagher P, Gallagher JP.

J Neurosci. 2005 Jan 19;25(3):577-83.


Distinct conformations of the corticotropin releasing factor type 1 receptor adopted following agonist and antagonist binding are differentially regulated.

Perry SJ, Junger S, Kohout TA, Hoare SR, Struthers RS, Grigoriadis DE, Maki RA.

J Biol Chem. 2005 Mar 25;280(12):11560-8. Epub 2005 Jan 14.


Modulation of dendritic differentiation by corticotropin-releasing factor in the developing hippocampus.

Chen Y, Bender RA, Brunson KL, Pomper JK, Grigoriadis DE, Wurst W, Baram TZ.

Proc Natl Acad Sci U S A. 2004 Nov 2;101(44):15782-7. Epub 2004 Oct 20.


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.


Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor.

Sullivan SK, Petroski RE, Verge G, Gross RS, Foster AC, Grigoriadis DE.

J Pharmacol Exp Ther. 2004 Nov;311(2):537-46. Epub 2004 Jul 15.


CRF receptor type 1 and 2 expression and anatomical distribution in the rat colon.

Chatzaki E, Crowe PD, Wang L, Million M, Taché Y, Grigoriadis DE.

J Neurochem. 2004 Jul;90(2):309-16.


Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.

Huang CQ, Wilcoxen KM, Grigoriadis DE, McCarthy JR, Chen C.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3943-7.


Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.

Webb TR, Moran T, Huang CQ, McCarthy JR, Grigoriadis DE, Chen C.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3869-73.


Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.

Chen C, Wilcoxen KM, Huang CQ, McCarthy JR, Chen T, Grigoriadis DE.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3669-73.


Conformational states of the corticotropin releasing factor 1 (CRF1) receptor: detection, and pharmacological evaluation by peptide ligands.

Hoare SR, Sullivan SK, Pahuja A, Ling N, Crowe PD, Grigoriadis DE.

Peptides. 2003 Dec;24(12):1881-97.


Corticotropin-releasing factor and Urocortin I modulate excitatory glutamatergic synaptic transmission.

Liu J, Yu B, Neugebauer V, Grigoriadis DE, Rivier J, Vale WW, Shinnick-Gallagher P, Gallagher JP.

J Neurosci. 2004 Apr 21;24(16):4020-9.


Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.

Huang CQ, Grigoriadis DE, Liu Z, McCarthy JR, Ramphal J, Webb T, Whitten JP, Xie MY, Chen C.

Bioorg Med Chem Lett. 2004 May 3;14(9):2083-6.


Ligand affinity for amino-terminal and juxtamembrane domains of the corticotropin releasing factor type I receptor: regulation by G-protein and nonpeptide antagonists.

Hoare SR, Sullivan SK, Schwarz DA, Ling N, Vale WW, Crowe PD, Grigoriadis DE.

Biochemistry. 2004 Apr 6;43(13):3996-4011.


Differential profile of CRF receptor distribution in the rat stomach and duodenum assessed by newly developed CRF receptor antibodies.

Chatzaki E, Murphy BJ, Wang L, Million M, Ohning GV, Crowe PD, Petroski R, Taché Y, Grigoriadis DE.

J Neurochem. 2004 Jan;88(1):1-11.


A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats.

Million M, Grigoriadis DE, Sullivan S, Crowe PD, McRoberts JA, Zhou H, Saunders PR, Maillot C, Mayer EA, Taché Y.

Brain Res. 2003 Sep 19;985(1):32-42.


Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.

Huang CQ, Wilcoxen K, McCarthy JR, Haddach M, Webb TR, Gu J, Xie YF, Grigoriadis DE, Chen C.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3375-9.


International Union of Pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ligands.

Hauger RL, Grigoriadis DE, Dallman MF, Plotsky PM, Vale WW, Dautzenberg FM.

Pharmacol Rev. 2003 Mar;55(1):21-6. Review.


Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists.

Hoare SR, Sullivan SK, Ling N, Crowe PD, Grigoriadis DE.

Mol Pharmacol. 2003 Mar;63(3):751-65. Erratum in: Mol Pharmacol. 2005 Jul;68(1):260.


Developing novel treatments for mood disorders: accelerating discovery.

Tamminga CA, Nemeroff CB, Blakely RD, Brady L, Carter CS, Davis KL, Dingledine R, Gorman JM, Grigoriadis DE, Henderson DC, B Innis RB, Killen J, Laughren TP, McDonald WM, M Murphy GM Jr, Paul SM, Rudorfer MV, Sausville E, Schatzberg AF, Scolnick EM, Suppes T.

Biol Psychiatry. 2002 Sep 15;52(6):589-609. Review.


Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist.

Heinrichs SC, De Souza EB, Schulteis G, Lapsansky JL, Grigoriadis DE.

Neuropsychopharmacology. 2002 Aug;27(2):194-202.

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