Xanomeline and the Antipsychotic Potential of Muscarinic Receptor Subtype Selective Agonists
نویسندگان
چکیده
منابع مشابه
Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists.
Binding studies initially suggested that the muscarinic agonist, xanomeline, was a subtype selective muscarinic M(1) receptor agonist, and a potential new treatment for Alzheimer's disease. However, later in vitro and in vivo functional studies suggest that this compound is probably better described as a subtype selective M(1)/M(4) muscarinic receptor agonist. This subtype selectivity profile h...
متن کاملThe muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat.
The muscarinic receptor agonist xanomeline was examined and compared with the antipsychotics clozapine and/or haloperidol in the following in vivo rat models: apomorphine-induced disruption of prepulse inhibition (PPI), amphetamine-induced hyperlocomotion, and the conditioned emotional response (CER) test. The effects of xanomeline were also assessed ex vivo on dopamine turnover in the rat medi...
متن کاملDesign of subtype selective melatonin receptor agonists and antagonists.
Studies of the physiological actions of melatonin have been hindered by the lack of specific, potent and subtype selective agonists and antagonists. In the present study, we describe the utility of a melanophore cell line from Xenopus laevis for exploring structure-activity relationships among novel melatonin analogues and report a novel MT2-selective agonist (IIK7) and MT2-selective receptor a...
متن کاملMuscarinic Receptor Agonists and Antagonists
A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed. A selection of chemical routes are described, which illustrate contemporary methodology for the synthes...
متن کاملInvolvement of a subpopulation of neuronal M4 muscarinic acetylcholine receptors in the antipsychotic-like effects of the M1/M4 preferring muscarinic receptor agonist xanomeline.
Disturbances in central dopaminergic neurotransmission are believed to be centrally involved in the pathogenesis of schizophrenia. Central dopaminergic and cholinergic systems interact and the cholinergic muscarinic agonist xanomeline has shown antipsychotic effects in clinical studies. Preclinical studies indicate that the M(4) muscarinic cholinergic receptor subtype (mAChR) modulates the acti...
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ژورنال
عنوان ژورنال: CNS Drug Reviews
سال: 2006
ISSN: 1080-563X
DOI: 10.1111/j.1527-3458.2003.tb00247.x