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Items: 1 to 50 of 55

1.

Structure-activity relationships for negative allosteric mGluR5 modulators.

Kaae BH, Harpsøe K, Kvist T, Mathiesen JM, Mølck C, Gloriam D, Jimenez HN, Uberti MA, Nielsen SM, Nielsen B, Bräuner-Osborne H, Sauerberg P, Clausen RP, Madsen U.

ChemMedChem. 2012 Mar 5;7(3):440-51. doi: 10.1002/cmdc.201100578. Epub 2012 Jan 20.

PMID:
22267204
2.

PPARδ agonists have opposing effects on insulin resistance in high fat-fed rats and mice due to different metabolic responses in muscle.

Ye JM, Tid-Ang J, Turner N, Zeng XY, Li HY, Cooney GJ, Wulff EM, Sauerberg P, Kraegen EW.

Br J Pharmacol. 2011 Jun;163(3):556-66. doi: 10.1111/j.1476-5381.2011.01240.x.

3.

Improved insulin sensitivity and islet function after PPARdelta activation in diabetic db/db mice.

Winzell MS, Wulff EM, Olsen GS, Sauerberg P, Gotfredsen CF, Ahrén B.

Eur J Pharmacol. 2010 Jan 25;626(2-3):297-305. doi: 10.1016/j.ejphar.2009.09.053. Epub 2009 Oct 8.

PMID:
19818749
4.

Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-gamma) agonist balaglitazone.

Larsen PJ, Lykkegaard K, Larsen LK, Fleckner J, Sauerberg P, Wassermann K, Wulff EM.

Eur J Pharmacol. 2008 Oct 31;596(1-3):173-9. doi: 10.1016/j.ejphar.2008.08.004. Epub 2008 Aug 16.

PMID:
18761337
5.

Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites.

Kaae BH, Harpsøe K, Kastrup JS, Sanz AC, Pickering DS, Metzler B, Clausen RP, Gajhede M, Sauerberg P, Liljefors T, Madsen U.

Chem Biol. 2007 Nov;14(11):1294-303.

6.

Design of a partial PPARdelta agonist.

Pettersson I, Ebdrup S, Havranek M, Pihera P, Korínek M, Mogensen JP, Jeppesen CB, Johansson E, Sauerberg P.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4625-9. Epub 2007 May 27.

PMID:
17560785
7.

Novel selective PPARdelta agonists: optimization of activity by modification of alkynylallylic moiety.

Havranek M, Sauerberg P, Mogensen JP, Kratina P, Jeppesen CB, Pettersson I, Pihera P.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4144-9. Epub 2007 May 21.

PMID:
17553681
8.

Design of potent PPARalpha agonists.

Sauerberg P, Mogensen JP, Jeppesen L, Bury PS, Fleckner J, Olsen GS, Jeppesen CB, Wulff EM, Pihera P, Havranek M, Polivka Z, Pettersson I.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3198-202. Epub 2007 Mar 12.

PMID:
17379517
9.

Identification and synthesis of a novel selective partial PPARdelta agonist with full efficacy on lipid metabolism in vitro and in vivo.

Sauerberg P, Olsen GS, Jeppesen L, Mogensen JP, Pettersson I, Jeppesen CB, Daugaard JR, Galsgaard ED, Ynddal L, Fleckner J, Panajotova V, Polivka Z, Pihera P, Havranek M, Wulff EM.

J Med Chem. 2007 Apr 5;50(7):1495-503. Epub 2007 Mar 8.

PMID:
17343371
10.

Selective PPAR agonists for the treatment of type 2 diabetes.

Nehlin JO, Mogensen JP, Petterson I, Jeppesen L, Fleckner J, Wulff EM, Sauerberg P.

Ann N Y Acad Sci. 2006 May;1067:448-53. Review.

PMID:
16804025
11.

Structure-activity relationships of dimeric PPAR agonists.

Sauerberg P, Mogensen JP, Jeppesen L, Svensson LA, Fleckner J, Nehlin J, Wulff EM, Pettersson I.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1497-500.

PMID:
15713415
12.

Prediction of PPAR-alpha ligand-mediated physiological changes using gene expression profiles.

Frederiksen KS, Wulff EM, Sauerberg P, Mogensen JP, Jeppesen L, Fleckner J.

J Lipid Res. 2004 Mar;45(3):592-601.

13.

Large dimeric ligands with favorable pharmacokinetic properties and peroxisome proliferator-activated receptor agonist activity in vitro and in vivo.

Sauerberg P, Bury PS, Mogensen JP, Deussen HJ, Pettersson I, Fleckner J, Nehlin J, Frederiksen KS, Albrektsen T, Din N, Svensson LA, Ynddal L, Wulff EM, Jeppesen L.

J Med Chem. 2003 Nov 6;46(23):4883-94.

PMID:
14584939
14.

Identification of hepatic transcriptional changes in insulin-resistant rats treated with peroxisome proliferator activated receptor-alpha agonists.

Frederiksen KS, Wulf EM, Wassermann K, Sauerberg P, Fleckner J.

J Mol Endocrinol. 2003 Jun;30(3):317-29.

PMID:
12790802
15.

Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.

Ebdrup S, Pettersson I, Rasmussen HB, Deussen HJ, Frost Jensen A, Mortensen SB, Fleckner J, Pridal L, Nygaard L, Sauerberg P.

J Med Chem. 2003 Apr 10;46(8):1306-17.

PMID:
12672231
16.

Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.

Mogensen JP, Jeppesen L, Bury PS, Pettersson I, Fleckner J, Nehlin J, Frederiksen KS, Albrektsen T, Din N, Mortensen SB, Svensson LA, Wassermann K, Wulff EM, Ynddal L, Sauerberg P.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):257-60.

PMID:
12482434
17.

Dual PPARalpha /gamma activation provides enhanced improvement of insulin sensitivity and glycemic control in ZDF rats.

Brand CL, Sturis J, Gotfredsen CF, Fleckner J, Fledelius C, Hansen BF, Andersen B, Ye JM, Sauerberg P, Wassermann K.

Am J Physiol Endocrinol Metab. 2003 Apr;284(4):E841-54. Epub 2002 Dec 10.

18.

Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.

Sauerberg P, Pettersson I, Jeppesen L, Bury PS, Mogensen JP, Wassermann K, Brand CL, Sturis J, Wöldike HF, Fleckner J, Andersen AS, Mortensen SB, Svensson LA, Rasmussen HB, Lehmann SV, Polivka Z, Sindelar K, Panajotova V, Ynddal L, Wulff EM.

J Med Chem. 2002 Feb 14;45(4):789-804.

PMID:
11831892
19.

Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.

Christopoulos A, Grant MK, Ayoubzadeh N, Kim ON, Sauerberg P, Jeppesen L, El-Fakahany EE.

J Pharmacol Exp Ther. 2001 Sep;298(3):1260-8.

PMID:
11504829
20.

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
21.

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
22.

Central muscarinic inhibition of lower urinary tract nociception.

Thor KB, Muhlhauser MA, Sauerberg P, Shannon H, Springer JP.

Brain Res. 2000 Jul 7;870(1-2):126-34.

PMID:
10869509
23.

Xanomeline, an M(1)/M(4) preferring muscarinic cholinergic receptor agonist, produces antipsychotic-like activity in rats and mice.

Shannon HE, Rasmussen K, Bymaster FP, Hart JC, Peters SC, Swedberg MD, Jeppesen L, Sheardown MJ, Sauerberg P, Fink-Jensen A.

Schizophr Res. 2000 May 5;42(3):249-59.

PMID:
10785583
24.

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
25.

Increased insulin secretion and normalization of glucose tolerance by cholinergic agonism in high fat-fed mice.

Ahrén B, Sauerberg P, Thomsen C.

Am J Physiol. 1999 Jul;277(1):E93-102. doi: 10.1152/ajpendo.1999.277.1.E93.

PMID:
10409132
26.

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
27.

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
28.

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
29.

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
30.

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
31.

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
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.

Effects of the M1 agonist xanomeline on processing of human beta-amyloid precursor protein (FAD, Swedish mutant) transfected into Chinese hamster ovary-m1 cells.

DeLapp N, Wu S, Belagaje R, Johnstone E, Little S, Shannon H, Bymaster F, Calligaro D, Mitch C, Whitesitt C, Ward J, Sheardown M, Fink-Jensen A, Jeppesen L, Thomsen C, Sauerberg P.

Biochem Biophys Res Commun. 1998 Mar 6;244(1):156-60.

PMID:
9514902
34.

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
35.

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
36.

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
37.

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
38.

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
39.

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
40.

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
41.

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
42.

PET study of the M1-agonists [11C]xanomeline and [11C]butylthio-TZTP in monkey and man.

Farde L, Suhara T, Halldin C, Nybäck H, Nakashima Y, Swahn CG, Karlsson P, Ginovart N, Bymaster FP, Shannon HE, Foged C, Suzdak PD, Sauerberg P.

Dementia. 1996 Jul-Aug;7(4):187-95.

PMID:
8835881
43.

1,2,5-Thiadiazole derivatives of arecoline stimulate M1 receptors coupled to phosphoinositide turnover.

Periyasamy S, Messer WS Jr, Roknich S, Sauerberg P, Hoss W.

Brain Res. 1995 Sep 25;693(1-2):118-23.

PMID:
8653399
44.

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
45.

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
46.

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
47.

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
48.

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
49.

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
50.

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