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Items: 1 to 20 of 99

1.

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
2.

Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.

Cao Y, Zhang M, Wu C, Lee S, Wroblewski ME, Whipple T, Nagy PI, Takács-Novák K, Balázs A, Torös S, Messer WS Jr.

J Med Chem. 2003 Sep 25;46(20):4273-86.

PMID:
13678406
3.

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
4.

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
6.

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
7.

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
8.

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
9.

Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.

Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM.

Br J Pharmacol. 1998 Dec;125(7):1413-20.

10.

6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.

Pei XF, Gupta TH, Badio B, Padgett WL, Daly JW.

J Med Chem. 1998 Jun 4;41(12):2047-55.

PMID:
9622546
12.

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
13.

Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.

Kane BE, Grant MK, El-Fakahany EE, Ferguson DM.

Bioorg Med Chem. 2008 Feb 1;16(3):1376-92. Epub 2007 Oct 22.

PMID:
17977730
14.

Differences in kinetics of xanomeline binding and selectivity of activation of G proteins at M(1) and M(2) muscarinic acetylcholine receptors.

Jakubík J, El-Fakahany EE, Dolezal V.

Mol Pharmacol. 2006 Aug;70(2):656-66. Epub 2006 May 4.

PMID:
16675658
15.

6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.

Daly JW, Gupta TH, Padgett WL, Pei XF.

J Med Chem. 2000 Jun 29;43(13):2514-22.

PMID:
10891110
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.

Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.

Rajeswaran WG, Cao Y, Huang XP, Wroblewski ME, Colclough T, Lee S, Liu F, Nagy PI, Ellis J, Levine BA, Nocka KH, Messer WS Jr.

J Med Chem. 2001 Dec 20;44(26):4563-76.

PMID:
11741475
18.

Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.

Sabb AL, Husbands GM, Tokolics J, Stein RP, Tasse RP, Boast CA, Moyer JA, Abou-Gharbia M.

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1895-900.

PMID:
10450949
19.

Wash-resistantly bound xanomeline inhibits acetylcholine release by persistent activation of presynaptic M(2) and M(4) muscarinic receptors in rat brain.

Machová E, Jakubík J, El-Fakahany EE, Dolezal V.

J Pharmacol Exp Ther. 2007 Jul;322(1):316-23. Epub 2007 Apr 19.

PMID:
17446301
20.

On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor.

Christopoulos A, Pierce TL, Sorman JL, El-Fakahany EE.

Mol Pharmacol. 1998 Jun;53(6):1120-30.

PMID:
9614217

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