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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. Sauerberg P, et al. Among authors: bymaster fp. J Med Chem. 1998 Jan 1;41(1):109-16. doi: 10.1021/jm9705216. J Med Chem. 1998. PMID: 9438027
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. Ward JS, et al. Among authors: bymaster fp. J Med Chem. 1998 Jan 29;41(3):379-92. doi: 10.1021/jm970125n. J Med Chem. 1998. PMID: 9464368
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. Sauerberg P, et al. Among authors: bymaster fp. J Med Chem. 1998 Oct 22;41(22):4378-84. doi: 10.1021/jm981048e. J Med Chem. 1998. PMID: 9784113
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. Jeppesen L, et al. Among authors: bymaster fp. J Med Chem. 1999 Jun 3;42(11):1999-2006. doi: 10.1021/jm9910019. J Med Chem. 1999. PMID: 10354408
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. Rasmussen T, et al. Among authors: bymaster fp. Eur J Pharmacol. 2000 Aug 25;402(3):241-6. doi: 10.1016/s0014-2999(00)00442-8. Eur J Pharmacol. 2000. PMID: 10958890
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