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Items: 1 to 50 of 59

1.

Preclinical predictors that the orthosteric mGlu2/3 receptor antagonist LY3020371 will not engender ketamine-associated neurotoxic, motor, cognitive, subjective, or abuse-liability-related effects.

Witkin JM, Monn JA, Li J, Johnson B, McKinzie DL, Wang XS, Heinz BA, Li R, Ornstein PL, Smith SC, Mitch CH, Calligaro DO, Swanson S, Allen D, Phillips K, Gilmour G.

Pharmacol Biochem Behav. 2017 Apr;155:43-55. doi: 10.1016/j.pbb.2017.03.001. Epub 2017 Mar 8.

PMID:
28285123
2.

The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans.

May PC, Willis BA, Lowe SL, Dean RA, Monk SA, Cocke PJ, Audia JE, Boggs LN, Borders AR, Brier RA, Calligaro DO, Day TA, Ereshefsky L, Erickson JA, Gevorkyan H, Gonzales CR, James DE, Jhee SS, Komjathy SF, Li L, Lindstrom TD, Mathes BM, Martényi F, Sheehan SM, Stout SL, Timm DE, Vaught GM, Watson BM, Winneroski LL, Yang Z, Mergott DJ.

J Neurosci. 2015 Jan 21;35(3):1199-210. doi: 10.1523/JNEUROSCI.4129-14.2015.

3.

A review of the abuse potential assessment of atomoxetine: a nonstimulant medication for attention-deficit/hyperactivity disorder.

Upadhyaya HP, Desaiah D, Schuh KJ, Bymaster FP, Kallman MJ, Clarke DO, Durell TM, Trzepacz PT, Calligaro DO, Nisenbaum ES, Emmerson PJ, Schuh LM, Bickel WK, Allen AJ.

Psychopharmacology (Berl). 2013 Mar;226(2):189-200. doi: 10.1007/s00213-013-2986-z. Epub 2013 Feb 9. Review.

4.

CNS distribution of metabotropic glutamate 2 and 3 receptors: transgenic mice and [³H]LY459477 autoradiography.

Wright RA, Johnson BG, Zhang C, Salhoff C, Kingston AE, Calligaro DO, Monn JA, Schoepp DD, Marek GJ.

Neuropharmacology. 2013 Mar;66:89-98. doi: 10.1016/j.neuropharm.2012.01.019. Epub 2012 Jan 31.

PMID:
22313530
5.

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor.

May PC, Dean RA, Lowe SL, Martenyi F, Sheehan SM, Boggs LN, Monk SA, Mathes BM, Mergott DJ, Watson BM, Stout SL, Timm DE, Smith Labell E, Gonzales CR, Nakano M, Jhee SS, Yen M, Ereshefsky L, Lindstrom TD, Calligaro DO, Cocke PJ, Greg Hall D, Friedrich S, Citron M, Audia JE.

J Neurosci. 2011 Nov 16;31(46):16507-16. doi: 10.1523/JNEUROSCI.3647-11.2011.

6.

Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan.

Nelson DL, Phebus LA, Johnson KW, Wainscott DB, Cohen ML, Calligaro DO, Xu YC.

Cephalalgia. 2010 Oct;30(10):1159-69. doi: 10.1177/0333102410370873. Epub 2010 Jun 15.

PMID:
20855361
7.

Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.

Krushinski JH Jr, Schaus JM, Thompson DC, Calligaro DO, Nelson DL, Luecke SH, Wainscott DB, Wong DT.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5600-4. Epub 2007 Aug 22.

PMID:
17804228
8.

Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039).

Rorick-Kehn LM, Johnson BG, Burkey JL, Wright RA, Calligaro DO, Marek GJ, Nisenbaum ES, Catlow JT, Kingston AE, Giera DD, Herin MF, Monn JA, McKinzie DL, Schoepp DD.

J Pharmacol Exp Ther. 2007 Apr;321(1):308-17. Epub 2007 Jan 4.

PMID:
17204749
9.

Pharmacological characterization of the competitive GLUK5 receptor antagonist decahydroisoquinoline LY466195 in vitro and in vivo.

Weiss B, Alt A, Ogden AM, Gates M, Dieckman DK, Clemens-Smith A, Ho KH, Jarvie K, Rizkalla G, Wright RA, Calligaro DO, Schoepp D, Mattiuz EL, Stratford RE, Johnson B, Salhoff C, Katofiasc M, Phebus LA, Schenck K, Cohen M, Filla SA, Ornstein PL, Johnson KW, Bleakman D.

J Pharmacol Exp Ther. 2006 Aug;318(2):772-81. Epub 2006 May 11.

PMID:
16690725
10.

In vitro and in vivo studies in rats with LY293558 suggest AMPA/kainate receptor blockade as a novel potential mechanism for the therapeutic treatment of anxiety disorders.

Alt A, Weiss B, Ogden AM, Li X, Gleason SD, Calligaro DO, Bleakman D, Witkin JM.

Psychopharmacology (Berl). 2006 Apr;185(2):240-7. Epub 2006 Feb 10.

PMID:
16470401
11.

Preclinical pharmacology of FMPD [6-fluoro-10-[3-(2-methoxyethyl)-4-methyl-piperazin-1-yl]-2-methyl-4H-3-thia-4,9-diaza-benzo[f]azulene]: a potential novel antipsychotic with lower histamine H1 receptor affinity than olanzapine.

Rasmussen K, Benvenga MJ, Bymaster FP, Calligaro DO, Cohen IR, Falcone JF, Hemrick-Luecke SK, Martin FM, Moore NA, Nisenbaum LK, Schaus JM, Sundquist SJ, Tupper DE, Wiernicki TR, Nelson DL.

J Pharmacol Exp Ther. 2005 Dec;315(3):1265-77. Epub 2005 Sep 1.

PMID:
16141369
12.

Muscarinic mechanisms of antipsychotic atypicality.

Bymaster FP, Felder CC, Tzavara E, Nomikos GG, Calligaro DO, Mckinzie DL.

Prog Neuropsychopharmacol Biol Psychiatry. 2003 Oct;27(7):1125-43. Review.

PMID:
14642972
13.

Adipsin, a biomarker of gastrointestinal toxicity mediated by a functional gamma-secretase inhibitor.

Searfoss GH, Jordan WH, Calligaro DO, Galbreath EJ, Schirtzinger LM, Berridge BR, Gao H, Higgins MA, May PC, Ryan TP.

J Biol Chem. 2003 Nov 14;278(46):46107-16. Epub 2003 Aug 29.

14.

A current review of olanzapine's safety in the geriatric patient: from pre-clinical pharmacology to clinical data.

Kennedy JS, Bymaster FP, Schuh L, Calligaro DO, Nomikos G, Felder CC, Bernauer M, Kinon BJ, Baker RW, Hay D, Roth HJ, Dossenbach M, Kaiser C, Beasley CM, Holcombe JH, Effron MB, Breier A.

Int J Geriatr Psychiatry. 2001 Dec;16 Suppl 1:S33-61. Review.

PMID:
11748788
15.

N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.

Xu YC, Johnson KW, Phebus LA, Cohen M, Nelson DL, Schenck K, Walker CD, Fritz JE, Kaldor SW, LeTourneau ME, Murff RE, Zgombick JM, Calligaro DO, Audia JE, Schaus JM.

J Med Chem. 2001 Nov 22;44(24):4031-4.

PMID:
11708905
16.

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
17.

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
18.

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
19.

The novel 5-Hydroxytryptamine(1A) antagonist LY426965: effects on nicotine withdrawal and interactions with fluoxetine.

Rasmussen K, Calligaro DO, Czachura JF, Dreshfield-Ahmad LJ, Evans DC, Hemrick-Luecke SK, Kallman MJ, Kendrick WT, Leander JD, Nelson DL, Overshiner CD, Wainscott DB, Wolff MC, Wong DT, Branchek TA, Zgombick JM, Xu YC.

J Pharmacol Exp Ther. 2000 Aug;294(2):688-700.

PMID:
10900249
20.

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
21.
22.

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
23.

Direct pharmacological comparison of the muscarinic receptors mediating relaxation and contraction in the rabbit thoracic aorta.

Sawyer BD, Bymaster FP, Calligaro DO, Falcone J, Mitch CH, Ward JS, Whitesitt C, Shannon HE.

Gen Pharmacol. 1999 Apr;32(4):445-52.

PMID:
10323485
24.

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
25.

Olanzapine: a basic science update.

Bymaster F, Perry KW, Nelson DL, Wong DT, Rasmussen K, Moore NA, Calligaro DO.

Br J Psychiatry Suppl. 1999;(37):36-40. Review.

PMID:
10211140
26.

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
27.

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
28.

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
29.

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
30.

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
31.

Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives.

Schaus JM, Thompson DC, Bloomquist WE, Susemichel AD, Calligaro DO, Cohen ML.

J Med Chem. 1998 May 21;41(11):1943-55.

PMID:
9599243
32.

Xanomeline compared to other muscarinic agents on stimulation of phosphoinositide hydrolysis in vivo and other cholinomimetic effects.

Bymaster FP, Carter PA, Peters SC, Zhang W, Ward JS, Mitch CH, Calligaro DO, Whitesitt CA, DeLapp N, Shannon HE, Rimvall K, Jeppesen L, Sheardown MJ, Fink-Jensen A, Sauerberg P.

Brain Res. 1998 Jun 8;795(1-2):179-90.

PMID:
9622623
33.

1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.

Ward JS, Merritt L, Calligaro DO, Bymaster FP, Shannon HE, Mitch CH, Whitesitt C, Brunsting D, Sheardown MJ, Olesen PH, Swedberg MD, Jeppesen L, Sauerberg P.

J Med Chem. 1998 Jan 29;41(3):379-92.

PMID:
9464368
34.

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
35.

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
36.

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
37.

Muscarinic analgesics with potent and selective effects on the gastrointestinal tract: potential application for the treatment of irritable bowel syndrome.

Mitch CH, Brown TJ, Bymaster FP, Calligaro DO, Dieckman D, Merrit L, Peters SC, Quimby SJ, Shannon HE, Shipley LA, Ward JS, Hansen K, Olesen PH, Sauerberg P, Sheardown MJ, Swedberg MD, Suzdak P, Greenwood B.

J Med Chem. 1997 Feb 14;40(4):538-46.

PMID:
9046345
38.

Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.

Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer AD Jr, Branchek TA, Flaugh ME.

Life Sci. 1997;61(21):2117-26.

PMID:
9395253
39.

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.

40.

In vivo pharmacology of butylthio[2.2.2] (LY297802 / NNC11-1053), an orally acting antinociceptive muscarinic agonist.

Shannon HE, Womer DE, Bymaster FP, Calligaro DO, DeLapp NC, Mitch CH, Ward JS, Whitesitt CA, Swedberg MD, Sheardown MJ, Fink-Jensen A, Olesen PH, Rimvall K, Sauerberg P.

Life Sci. 1997;60(13-14):969-76. Review.

PMID:
9121363
41.

Radioreceptor binding profile of the atypical antipsychotic olanzapine.

Bymaster FP, Calligaro DO, Falcone JF, Marsh RD, Moore NA, Tye NC, Seeman P, Wong DT.

Neuropsychopharmacology. 1996 Feb;14(2):87-96.

42.

Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles.

Ward JS, Merritt L, Calligaro DO, Bymaster FP, Shannon HE, Sawyer BD, Mitch CH, Deeter JB, Peters SC, Sheardown MJ, Olesen PH, Swedberg MD, Sauerberg P.

J Med Chem. 1995 Sep 1;38(18):3469-81.

PMID:
7658434
43.

Muscarinic agonists as analgesics. Antinociceptive activity versus M1 activity: SAR of alkylthio-TZTP's and related 1,2,5-thiadiazole analogs.

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

Life Sci. 1995;56(11-12):807-14.

PMID:
10188779
44.

Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity.

Foreman MM, Fuller RW, Rasmussen K, Nelson DL, Calligaro DO, Zhang L, Barrett JE, Booher RN, Paget CJ Jr, Flaugh ME.

J Pharmacol Exp Ther. 1994 Sep;270(3):1270-81.

PMID:
7523657
45.

Neurochemical effects of the M1 muscarinic agonist xanomeline (LY246708/NNC11-0232).

Bymaster FP, Wong DT, Mitch CH, Ward JS, Calligaro DO, Schoepp DD, Shannon HE, Sheardown MJ, Olesen PH, Suzdak PD, Swedberg MD, Sauerberg P.

J Pharmacol Exp Ther. 1994 Apr;269(1):282-9.

PMID:
7909558
46.

Xanomeline: a novel muscarinic receptor agonist with functional selectivity for M1 receptors.

Shannon HE, Bymaster FP, Calligaro DO, Greenwood B, Mitch CH, Sawyer BD, Ward JS, Wong DT, Olesen PH, Sheardown MJ, Swedberg MD, Suzdak PD, Sauerberg P.

J Pharmacol Exp Ther. 1994 Apr;269(1):271-81.

PMID:
7909557
47.

Comparative 5-HT2-receptor antagonist activity of amesergide and its active metabolite 4-hydroxyamesergide in rats and rabbits.

Cohen ML, Kurz KD, Fuller RW, Calligaro DO.

J Pharm Pharmacol. 1994 Mar;46(3):226-9.

PMID:
8027933
48.

Preclinical studies on LY228729: a potent and selective serotonin1A agonist.

Foreman MM, Fuller RW, Leander JD, Benvenga MJ, Wong DT, Nelson DL, Calligaro DO, Swanson SP, Lucot JB, Flaugh ME.

J Pharmacol Exp Ther. 1993 Oct;267(1):58-71.

PMID:
8229788
49.

Allosteric regulation by sodium of the binding of [3H]cocaine and [3H]GBR 12935 to rat and bovine striata.

Eshleman AJ, Calligaro DO, Eldefrawi ME.

Membr Biochem. 1993 Jul-Sep;10(3):129-44.

PMID:
8231896
50.

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