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Items: 33

1.

An Allosteric Potentiator of the Dopamine D1 Receptor Increases Locomotor Activity in Human D1 Knock-In Mice without Causing Stereotypy or Tachyphylaxis.

Svensson KA, Heinz BA, Schaus JM, Beck JP, Hao J, Krushinski JH, Reinhard MR, Cohen MP, Hellman SL, Getman BG, Wang X, Menezes MM, Maren DL, Falcone JF, Anderson WH, Wright RA, Morin SM, Knopp KL, Adams BL, Rogovoy B, Okun I, Suter TM, Statnick MA, Gehlert DR, Nelson DL, Lucaites VL, Emkey R, DeLapp NW, Wiernicki TR, Cramer JW, Yang CR, Bruns RF.

J Pharmacol Exp Ther. 2017 Jan;360(1):117-128. Epub 2016 Nov 3.

2.

GTPγS Binding Assays.

DeLapp NW, Gough WH, Kahl SD, Porter AC, Wiernicki TR.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin CP, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Saradjian P, 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-.
2012 May 1 [updated 2012 Oct 1].

3.

Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats.

Arnt J, Bang-Andersen B, Grayson B, Bymaster FP, Cohen MP, DeLapp NW, Giethlen B, Kreilgaard M, McKinzie DL, Neill JC, Nelson DL, Nielsen SM, Poulsen MN, Schaus JM, Witten LM.

Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33. doi: 10.1017/S1461145710000659. Epub 2010 Jun 23.

PMID:
20569520
4.

The minimum significant ratio: a statistical parameter to characterize the reproducibility of potency estimates from concentration-response assays and estimation by replicate-experiment studies.

Eastwood BJ, Farmen MW, Iversen PW, Craft TJ, Smallwood JK, Garbison KE, Delapp NW, Smith GF.

J Biomol Screen. 2006 Apr;11(3):253-61. Epub 2006 Feb 20.

PMID:
16490778
5.

The antibody-capture [(35)S]GTPgammaS scintillation proximity assay: a powerful emerging technique for analysis of GPCR pharmacology.

DeLapp NW.

Trends Pharmacol Sci. 2004 Aug;25(8):400-1. Review. No abstract available.

PMID:
15276707
6.

M1 muscarinic receptor signaling in mouse hippocampus and cortex.

Porter AC, Bymaster FP, DeLapp NW, Yamada M, Wess J, Hamilton SE, Nathanson NM, Felder CC.

Brain Res. 2002 Jul 19;944(1-2):82-9.

PMID:
12106668
7.

Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapine.

Bymaster FP, Falcone JF, Bauzon D, Kennedy JS, Schenck K, DeLapp NW, Cohen ML.

Eur J Pharmacol. 2001 Nov 2;430(2-3):341-9.

PMID:
11711053
8.

Receptor reserve of phosphoinositide-coupled muscarinic receptors in mouse hippocampus in vivo.

Bymaster FP, Carter PA, DeLapp NW, Calligaro DO, Felder CC.

Brain Res. 2001 Oct 19;916(1-2):165-71.

PMID:
11597604
9.

The muscarinic receptor agonist BuTAC, a novel potential antipsychotic, does not impair learning and memory in mouse passive avoidance.

Rasmussen T, Fink-Jensen A, Sauerberg P, Swedberg MD, Thomsen C, Sheardown MJ, Jeppesen L, Calligaro DO, DeLapp NW, Whitesitt C, Ward JS, Shannon HE, Bymaster FP.

Schizophr Res. 2001 Apr 15;49(1-2):193-201.

PMID:
11343877
10.

Muscarinic receptor agonists decrease cocaine self-administration rates in drug-naive mice.

Rasmussen T, Sauerberg P, Nielsen EB, Swedberg MD, Thomsen C, Sheardown MJ, Jeppesen L, Calligaro DO, DeLapp NW, Whitesitt C, Ward JS, Shannon HE, Bymaster FP, Fink-Jensen A.

Eur J Pharmacol. 2000 Aug 25;402(3):241-6.

PMID:
10958890
11.

Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats.

Shannon HE, Hart JC, Bymaster FP, Calligaro DO, DeLapp NW, Mitch CH, Ward JS, Fink-Jensen A, Sauerberg P, Jeppesen L, Sheardown MJ, Swedberg MD.

J Pharmacol Exp Ther. 1999 Aug;290(2):901-7.

PMID:
10411607
12.

1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.

Jeppesen L, Olesen PH, Hansen L, Sheardown MJ, Thomsen C, Rasmussen T, Jensen AF, Christensen MS, Rimvall K, Ward JS, Whitesitt C, Calligaro DO, Bymaster FP, Delapp NW, Felder CC, Shannon HE, Sauerberg P.

J Med Chem. 1999 Jun 3;42(11):1999-2006.

PMID:
10354408
13.

Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.

Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO.

Schizophr Res. 1999 May 4;37(1):107-22.

PMID:
10227113
14.
15.

Potential role of muscarinic receptors in schizophrenia.

Bymaster FP, Shannon HE, Rasmussen K, DeLapp NW, Ward JS, Calligaro DO, Mitch CH, Whitesitt C, Ludvigsen TS, Sheardown M, Swedberg M, Rasmussen T, Olesen PH, Jeppesen L, Sauerberg P, Fink-Jensen A.

Life Sci. 1999;64(6-7):527-34.

PMID:
10069519
16.

Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.

Sauerberg P, Jeppesen L, Olesen PH, Sheardown MJ, Fink-Jensen A, Rasmussen T, Rimvall K, Shannon HE, Bymaster FP, DeLapp NW, Calligaro DO, Ward JS, Whitesitt CA, Thomsen C.

Bioorg Med Chem Lett. 1998 Oct 20;8(20):2897-902.

PMID:
9873644
17.

Muscarinic agonists exhibit functional dopamine antagonism in unilaterally 6-OHDA lesioned rats.

Fink-Jensen A, Kristensen P, Shannon HE, Calligaro DO, Delapp NW, Whitesitt C, Ward JS, Thomsen C, Rasmusseen T, Sheardown MJ, Jeppesen L, Sauerberg P, Bymaster FP.

Neuroreport. 1998 Oct 26;9(15):3481-6. Erratum in: Neuroreport 1998 Nov 16;9(16):inside back cov.

PMID:
9855303
18.

Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.

Sauerberg P, Jeppesen L, Olesen PH, Rasmussen T, Swedberg MD, Sheardown MJ, Fink-Jensen A, Thomsen C, Thøgersen H, Rimvall K, Ward JS, Calligaro DO, DeLapp NW, Bymaster FP, Shannon HE.

J Med Chem. 1998 Oct 22;41(22):4378-84.

PMID:
9784113
19.

Unexpected antipsychotic-like activity with the muscarinic receptor ligand (5R,6R)6-(3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicyclo[3.2.1]octane .

Bymaster FP, Shannon HE, Rasmussen K, Delapp NW, Mitch CH, Ward JS, Calligaro DO, Ludvigsen TS, Sheardown MJ, Olesen PH, Swedberg MD, Sauerberg P, Fink-Jensen A.

Eur J Pharmacol. 1998 Sep 4;356(2-3):109-19.

PMID:
9774240
20.

Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.

Sauerberg P, Olesen PH, Sheardown MJ, Rimvall K, Thøgersen H, Shannon HE, Sawyer BD, Ward JS, Bymaster FP, DeLapp NW, Calligaro DO, Swedberg MD.

J Med Chem. 1998 Jan 1;41(1):109-16.

PMID:
9438027
21.

Pharmacology of butylthio[2.2.2] (LY297802/NNC11-1053): a novel analgesic with mixed muscarinic receptor agonist and antagonist activity.

Shannon HE, Sheardown MJ, Bymaster FP, Calligaro DO, Delapp NW, Gidda J, Mitch CH, Sawyer BD, Stengel PW, Ward JS, Wong DT, Olesen PH, Suzdak PD, Sauerberg P, Swedberg MD.

J Pharmacol Exp Ther. 1997 May;281(2):884-94.

PMID:
9152398
22.

Butylthio[2.2.2] (NNC 11-1053/LY297802): an orally active muscarinic agonist analgesic.

Swedberg MD, Sheardown MJ, Sauerberg P, Olesen PH, Suzdak PD, Hansen KT, Bymaster FP, Ward JS, Mitch CH, Calligaro DO, Delapp NW, Shannon HE.

J Pharmacol Exp Ther. 1997 May;281(2):876-83.

PMID:
9152397
23.

Intrathecal pertussis toxin produces hyperalgesia and allodynia in mice.

Womer DE, DeLapp NW, Shannon HE.

Pain. 1997 Apr;70(2-3):223-8.

PMID:
9150297
24.

In vitro and in vivo biochemistry of olanzapine: a novel, atypical antipsychotic drug.

Bymaster FP, Rasmussen K, Calligaro DO, Nelson DL, DeLapp NW, Wong DT, Moore NA.

J Clin Psychiatry. 1997;58 Suppl 10:28-36. Review.

25.
26.

The muscarinic M1 agonist xanomeline increases soluble amyloid precursor protein release from Chinese hamster ovary-m1 cells.

Eckols K, Bymaster FP, Mitch CH, Shannon HE, Ward JS, DeLapp NW.

Life Sci. 1995;57(12):1183-90.

PMID:
7674807
27.
29.

Gamma glutamyl peptidase: a novel enzyme from hairless mouse epidermis.

DeLapp NW, Dieckman DK.

J Invest Dermatol. 1988 Apr;90(4):490-4.

30.

Biosynthesis of pyrrolidone carboxylic acid in hairless mouse epidermis.

DeLapp NW, Dieckman DK.

J Invest Dermatol. 1977 May;68(5):293-8.

31.

Importance of pyrimidine nucleotide salvage pathways for DNA synthesis in skin.

DeLapp NW, Karasek MA.

J Invest Dermatol. 1976 May;66(5):306-12.

32.

Induction of chick liver xanthine dehydrogenase by purines.

Woodward WD, Lee PC, DeLapp NW, Fisher JR.

Arch Biochem Biophys. 1972 Dec;153(2):537-42. No abstract available.

PMID:
4662098
33.

Correlations of tissue oxypurine levels with xanthine dehydrogenase changes in the chick.

DeLapp NW, Fisher JR.

Biochim Biophys Acta. 1972 May 29;269(3):505-14. No abstract available.

PMID:
5039546

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