131987-70-7Relevant academic research and scientific papers
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation
Sauerberg, Per,Jeppesen, Lone,Olesen, Preben H.,Sheardown, Malcolm J.,Fink-Jensen, Anders,Rasmussen, Thoger,Rimvall, Karin,Shannon, Harlan E.,Bymaster, Frank P.,DeLapp, Neil W.,Calligaro, Dave O.,Ward, John S.,Whitesitt, Celia A.,Thomsen, Christian
, p. 2897 - 2902 (2007/10/03)
Series of analogs to the functional m1 selective agonist, xanomeline (hexyloxy-TZTP), were evaluated for their in vitro ml efficacy in cell lines transfected with the human m1 receptor. Systematic variation of the side chain and the azacyclic ring led to the discovery of potent muscarinic agonists with robust m1 efficacy, all having the phenylpropargyloxy/thio as the side chain. The most selective compound was the phenylpropargylthio- [3.2.1] endo analog 28, which is a potent and efficacious m1 agonist with no m2 activity.
METHOD OF TREATING SCHIZOPHRENIA
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, (2008/06/13)
The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases by administering thiadiazole or oxadiazole compounds.
METHOD OF TREATING GASTROINTESTINAL MOTILITY DISORDERS
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, (2008/06/13)
The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.
Method of treating urinary bladder dysfunctions with 3-tetrahydropyridine derivatives
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, (2008/06/13)
The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.
Piperidine compounds and their preparation and use
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, (2008/06/13)
The present invention relates to therapeutically active piperidine compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful as stimulants of the cognitive function of the forebra
