Selectivity M4 acceptor antagonist and medical use thereof

Abstract

The invention provides a selective M4 receptor antagonist--levorotation demethylation phencynonate, non-toxic medicine salt thereof, medical composition that contains the levorotation demethylation phencynonate and non-toxic salt as active ingredients and application thereof in preparation of therapeutic drugs for motility dysfunctions of fremitus, rigor, etc. caused by Parkinson's syndrome (PD).The structure of the composition is showed in formula IIa.

Description

technical field The present invention provides a new selective M4 receptor antagonist - L-desmethylphencyclonate and its non-toxic pharmaceutically acceptable salt, a pharmaceutical composition containing the compound as an active ingredient, and its use in Application in the preparation of therapeutic drugs for motor dysfunction such as tremor and stiffness caused by Parkinson's disease (PD). Background technique M choline receptor is a very important target for drug therapy. The dysfunction of smooth muscle regulated by M1 / M3 receptors, including chronic obstructive pulmonary disease and urinary incontinence, has become a high incidence worldwide; M2 receptors Antagonists boost the release of acetylcholine in the brain and are used in the treatment of Alzheimer's disease. M4 receptors can inhibit the adenylyl cyclase system, which mainly exists in the striatum, and play an important role in the pathogenesis and development of Parkinson's disease (PD). M4 receptor antagon...

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Problems solved by technology

No selective M4 receptor antagonists have been found

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