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Items: 48

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.

Comparative Effects of LY3020371, a Potent and Selective Metabotropic Glutamate (mGlu) 2/3 Receptor Antagonist, and Ketamine, a Noncompetitive N-Methyl-d-Aspartate Receptor Antagonist in Rodents: Evidence Supporting the Use of mGlu2/3 Antagonists, for the Treatment of Depression.

Witkin JM, Mitchell SN, Wafford KA, Carter G, Gilmour G, Li J, Eastwood BJ, Overshiner C, Li X, Rorick-Kehn L, Rasmussen K, Anderson WH, Nikolayev A, Tolstikov VV, Kuo MS, Catlow JT, Li R, Smith SC, Mitch CH, Ornstein PL, Swanson S, Monn JA.

J Pharmacol Exp Ther. 2017 Apr;361(1):68-86. doi: 10.1124/jpet.116.238121. Epub 2017 Jan 30.

PMID:
28138040
3.

Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.

Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL.

J Med Chem. 2016 Dec 22;59(24):10974-10993. Epub 2016 Dec 6.

PMID:
28002967
4.

Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.

Dressman BA, Tromiczak EG, Chappell MD, Tripp AE, Quimby SJ, Vetman T, Fivush AM, Matt J, Jaramillo C, Li R, Khilevich A, Blanco MJ, Smith SC, Carpintero M, de Diego JE, Barberis M, García-Cerrada S, Soriano JF, Schkeryantz JM, Witkin JM, Wafford KA, Seidel W, Britton T, Overshiner CD, Li X, Wang XS, Heinz BA, Catlow JT, Swanson S, Bedwell D, Ornstein PL, Mitch CH.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5663-5668. doi: 10.1016/j.bmcl.2016.10.067. Epub 2016 Oct 25.

PMID:
27836401
5.

In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist.

Witkin JM, Ornstein PL, Mitch CH, Li R, Smith SC, Heinz BA, Wang XS, Xiang C, Carter JH, Anderson WH, Li X, Broad LM, Pasqui F, Fitzjohn SM, Sanger HE, Smith JL, Catlow J, Swanson S, Monn JA.

Neuropharmacology. 2017 Mar 15;115:100-114. doi: 10.1016/j.neuropharm.2015.12.021. Epub 2015 Dec 31.

PMID:
26748052
6.

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.

7.

Design, synthesis, and evaluation of hydroxamic acid-based molecular probes for in vivo imaging of histone deacetylase (HDAC) in brain.

Wang C, Eessalu TE, Barth VN, Mitch CH, Wagner FF, Hong Y, Neelamegam R, Schroeder FA, Holson EB, Haggarty SJ, Hooker JM.

Am J Nucl Med Mol Imaging. 2013 Dec 15;4(1):29-38. eCollection 2013.

8.

LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders.

Rorick-Kehn LM, Witkin JM, Statnick MA, Eberle EL, McKinzie JH, Kahl SD, Forster BM, Wong CJ, Li X, Crile RS, Shaw DB, Sahr AE, Adams BL, Quimby SJ, Diaz N, Jimenez A, Pedregal C, Mitch CH, Knopp KL, Anderson WH, Cramer JW, McKinzie DL.

Neuropharmacology. 2014 Feb;77:131-44. doi: 10.1016/j.neuropharm.2013.09.021. Epub 2013 Sep 23.

PMID:
24071566
9.

Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.

Mitch CH, Quimby SJ, Diaz N, Pedregal C, de la Torre MG, Jimenez A, Shi Q, Canada EJ, Kahl SD, Statnick MA, McKinzie DL, Benesh DR, Rash KS, Barth VN.

J Med Chem. 2011 Dec 8;54(23):8000-12. doi: 10.1021/jm200789r. Epub 2011 Oct 26.

PMID:
21958337
10.

Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation.

Melief EJ, Miyatake M, Carroll FI, Béguin C, Carlezon WA Jr, Cohen BM, Grimwood S, Mitch CH, Rorick-Kehn L, Chavkin C.

Mol Pharmacol. 2011 Nov;80(5):920-9. doi: 10.1124/mol.111.074195. Epub 2011 Aug 10.

11.

Activation of mesolimbic dopamine neurons during novel and daily limited access to palatable food is blocked by the opioid antagonist LY255582.

Sahr AE, Sindelar DK, Alexander-Chacko JT, Eastwood BJ, Mitch CH, Statnick MA.

Am J Physiol Regul Integr Comp Physiol. 2008 Aug;295(2):R463-71. doi: 10.1152/ajpregu.00390.2007. Epub 2008 Jun 4.

12.

Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.

Takeuchi K, Holloway WG, Mitch CH, Quimby SJ, McKinzie JH, Suter TM, Statnick MA, Surface PL, Emmerson PJ, Thomas EM, Siegel MG.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.

PMID:
17980586
13.

Effects of kappa opioid receptor agonists on attention as assessed by a 5-choice serial reaction time task in rats.

Shannon HE, Eberle EL, Mitch CH, McKinzie DL, Statnick MA.

Neuropharmacology. 2007 Dec;53(8):930-41. Epub 2007 Sep 20.

PMID:
17959202
14.

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.

PMID:
17935738
15.

Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.

Takeuchi K, Holloway WG, McKinzie JH, Suter TM, Statnick MA, Surface PL, Emmerson PJ, Thomas EM, Siegel MG, Matt JE, Wolfe CN, Mitch CH.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.

PMID:
17720493
16.

Localization of opioid receptor antagonist [3H]-LY255582 binding sites in mouse brain: comparison with the distribution of mu, delta and kappa binding sites.

Gackenheimer SL, Suter TM, Pintar JE, Quimby SJ, Wheeler WJ, Mitch CH, Gehlert DR, Statnick MA.

Neuropeptides. 2005 Dec;39(6):559-67. Epub 2005 Nov 9.

PMID:
16289278
17.

Na+ modulation, inverse agonism, and anorectic potency of 4-phenylpiperidine opioid antagonists.

Emmerson PJ, McKinzie JH, Surface PL, Suter TM, Mitch CH, Statnick MA.

Eur J Pharmacol. 2004 Jun 28;494(2-3):121-30.

PMID:
15212965
18.

Na+-dependent high affinity binding of [3H]LY515300, a 3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid receptor inverse agonist.

Statnick MA, Suter TM, Gackenheimer SL, Emmerson PJ, Quimby SJ, Gehlert DR, Wheeler WJ, Mitch CH.

Eur J Pharmacol. 2003 Dec 15;482(1-3):139-50.

PMID:
14660015
19.

Peptides that regulate food intake: antagonism of opioid receptors reduces body fat in obese rats by decreasing food intake and stimulating lipid utilization.

Statnick MA, Tinsley FC, Eastwood BJ, Suter TM, Mitch CH, Heiman ML.

Am J Physiol Regul Integr Comp Physiol. 2003 Jun;284(6):R1399-408.

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.

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
22.

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
23.

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
24.

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
25.

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
26.

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
27.

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
28.

M1 receptor agonist activity is not a requirement for muscarinic antinociception.

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

J Pharmacol Exp Ther. 1997 May;281(2):868-75.

PMID:
9152396
29.

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
30.

Synthesis and structural determination of stereoisomers of muscarinic ligands of the (3-propylthio-1,2,5-thiadiazol-4-yl)-1-azabicycloalkane type.

Olesen PH, Sauerberg P, Petersen TG, Treppendahl S, Bentzen B, Deeter J, Ward JS, Mitch CH, Lehmann SV.

Chirality. 1997;9(8):739-49.

PMID:
9435099
31.

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
32.

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
33.

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
34.

Novel alkoxy-oxazolyl-tetrahydropyridine muscarinic cholinergic receptor antagonists.

Shannon HE, Bymaster FP, Hendrix JC, Quimby SJ, Mitch CH.

Psychopharmacology (Berl). 1995 Jan;117(2):208-15.

PMID:
7753969
35.

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
36.

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
37.

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
38.

Use of the mouse vas deferens to determine mu, delta, and kappa receptor affinities of opioid antagonists.

Cohen ML, Mendelsohn LG, Mitch CH, Zimmerman DM.

Receptor. 1994 Spring;4(1):43-53.

PMID:
8038706
39.
40.

3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.

Mitch CH, Leander JD, Mendelsohn LG, Shaw WN, Wong DT, Cantrell BE, Johnson BG, Reel JK, Snoddy JD, Takemori AE, et al.

J Med Chem. 1993 Oct 1;36(20):2842-50.

PMID:
8410999
41.

Structure-activity relationships of trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine antagonists for mu- and kappa-opioid receptors.

Zimmerman DM, Leander JD, Cantrell BE, Reel JK, Snoddy J, Mendelsohn LG, Johnson BG, Mitch CH.

J Med Chem. 1993 Oct 1;36(20):2833-41.

PMID:
8410998
42.

Muscarinic M1 receptor agonist actions of muscarinic receptor agonists in rabbit vas deferens.

Shannon HE, Sawyer BD, Bemis KG, Bymaster FP, Health I, Mitch CH, Ward JS.

Eur J Pharmacol. 1993 Feb 23;232(1):47-57.

PMID:
8458395
43.

Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore.

Ward JS, Merritt L, Klimkowski VJ, Lamb ML, Mitch CH, Bymaster FP, Sawyer B, Shannon HE, Olesen PH, Honoré T, et al.

J Med Chem. 1992 Oct 30;35(22):4011-9.

PMID:
1433209
44.

Steric and electronic requirements for muscarinic receptor-stimulated phosphoinositide turnover in the CNS in a series of arecoline bioisosteres.

Ngur D, Roknich S, Mitch CH, Quimby SJ, Ward JS, Merritt L, Sauerberg P, Messer WS Jr, Hoss W.

Biochem Biophys Res Commun. 1992 Sep 30;187(3):1389-94.

PMID:
1329735
45.

Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.

McQuaid LA, Smith EC, South KK, Mitch CH, Schoepp DD, True RA, Calligaro DO, O'Malley PJ, Lodge D, Ornstein PL.

J Med Chem. 1992 Sep 4;35(18):3319-24.

PMID:
1382133
46.

Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines .

Sauerberg P, Olesen PH, Nielsen S, Treppendahl S, Sheardown MJ, Honoré T, Mitch CH, Ward JS, Pike AJ, Bymaster FP, et al.

J Med Chem. 1992 Jun 12;35(12):2274-83.

PMID:
1613751
47.

The effect of the opioid antagonist LY255582 on body weight of the obese Zucker rat.

Shaw WN, Mitch CH, Leander JD, Mendelsohn LG, Zimmerman DM.

Int J Obes. 1991 Jun;15(6):387-95.

PMID:
1653188
48.

Effect of phenylpiperidine opioid antagonists on food consumption and weight gain of the obese Zucker rat.

Shaw WN, Mitch CH, Leander JD, Zimmerman DM.

J Pharmacol Exp Ther. 1990 Apr;253(1):85-9.

PMID:
2329525

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