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Items: 12


In Vivo Receptor Occupancy in Rodents by LC-MS/MS.

Jesudason CD, DuBois S, Johnson M, Barth VN, Need AB.

In: Sittampalam GS, Coussens NP, Brimacombe K, Grossman A, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Inglese J, Iversen PW, Kahl SD, Kales SC, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2017 Mar 9.


Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.

Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM.

J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29.


Determining pharmacological selectivity of the kappa opioid receptor antagonist LY2456302 using pupillometry as a translational biomarker in rat and human.

Rorick-Kehn LM, Witcher JW, Lowe SL, Gonzales CR, Weller MA, Bell RL, Hart JC, Need AB, McKinzie JH, Statnick MA, Suico JG, McKinzie DL, Tauscher-Wisniewski S, Mitch CH, Stoltz RR, Wong CJ.

Int J Neuropsychopharmacol. 2014 Oct 31;18(2). pii: pyu036. doi: 10.1093/ijnp/pyu036.


Glucose metabolic trapping in mouse arteries: nonradioactive assay of atherosclerotic plaque inflammation applicable to drug discovery.

Conway RG, Chernet E, De Rosa DC, Benschop RJ, Need AB, Collins EC, Bean JS, Kalbfleisch JM, Rekhter MD.

PLoS One. 2012;7(11):e50349. doi: 10.1371/journal.pone.0050349. Epub 2012 Nov 28.


In vivo occupancy of dopamine D3 receptors by antagonists produces neurochemical and behavioral effects of potential relevance to attention-deficit-hyperactivity disorder.

Barth V, Need AB, Tzavara ET, Giros B, Overshiner C, Gleason SD, Wade M, Johansson AM, Perry K, Nomikos GG, Witkin JM.

J Pharmacol Exp Ther. 2013 Feb;344(2):501-10. doi: 10.1124/jpet.112.198895. Epub 2012 Nov 29.


In vivo rat brain opioid receptor binding of LY255582 assessed with a novel method using LC/MS/MS and the administration of three tracers simultaneously.

Need AB, McKinzie JH, Mitch CH, Statnick MA, Phebus LA.

Life Sci. 2007 Oct 13;81(17-18):1389-96. Epub 2007 Sep 19.


Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice.

Li X, Need AB, Baez M, Witkin JM.

J Pharmacol Exp Ther. 2006 Oct;319(1):254-9. Epub 2006 Jun 27.


Comparison of rat dopamine D2 receptor occupancy for a series of antipsychotic drugs measured using radiolabeled or nonlabeled raclopride tracer.

Barth VN, Chernet E, Martin LJ, Need AB, Rash KS, Morin M, Phebus LA.

Life Sci. 2006 May 22;78(26):3007-12. Epub 2006 Jan 24.


The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats.

Need AB, Davis RJ, Alexander-Chacko JT, Eastwood B, Chernet E, Phebus LA, Sindelar DK, Nomikos GG.

Psychopharmacology (Berl). 2006 Jan;184(1):26-35. Epub 2005 Nov 18.


Use of LC/MS to assess brain tracer distribution in preclinical, in vivo receptor occupancy studies: dopamine D2, serotonin 2A and NK-1 receptors as examples.

Chernet E, Martin LJ, Li D, Need AB, Barth VN, Rash KS, Phebus LA.

Life Sci. 2005 Dec 12;78(4):340-6. Epub 2005 Sep 1.


Enhancement of antidepressant potency by a potentiator of AMPA receptors.

Li X, Witkin JM, Need AB, Skolnick P.

Cell Mol Neurobiol. 2003 Jun;23(3):419-30.


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