131988-19-7Relevant articles and documents
Synthesis and evaluation of xanomeline analogs-Probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor
Kane, Brian E.,Grant, Marianne K.O.,El-Fakahany, Esam E.,Ferguson, David M.
, p. 1376 - 1392 (2008/09/18)
A series of xanomeline analogs were synthesized and evaluated for binding at the M1 muscarinic acetylcholine receptor (M1 receptor). Specifically, compounds that substitute the O-hexyl chain of xanomeline with polar, ionizable, or conformationally restricted moieties were assessed for their ability to bind to the M1 receptor in a wash-resistant manner (persistent binding). From our screen, several novel ligands that persistently bind to the M1 receptor with greater affinity than xanomeline were discovered. Results indicate that persistent binding may arise not only from hydrophobic interactions but also from ionic interactions with a secondary M1 receptor binding site. Herein, a qualitative model that accounts for both binding scenarios is proposed and applied to understand the structural basis to wash-resistant binding and long-acting effects of xanomeline-based compounds.
Combination therapy for treatment of psychoses
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, (2008/06/13)
The invention provides combination therapy comprising a first component which is a typical antipsychotic or an atypical antipsychotic and a second component which is a muscarinic agonist for the treatment of psychoses and other disorders.
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 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.
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.
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