VU0255035 is the first highly selective antagonist at the orthosteric site of the M1 receptor (75-fold selective for M1 relative to other muscarininc subtypes and devoid of activity at other GPCRs, ion channels, transporters and kinases).

VU0255035 is the first highly selective antagonist at the orthosteric site of the M1 receptor (75-fold selective for M1 relative to other muscarininc subtypes and devoid of activity at other GPCRs, ion channels, transporters and kinases). There are no highly selective M1 muscarinic receptor antagonists. The existing non-selective drugs do not permit direct evaluation of the role of M1 receptors in CNS fucntions and do not premit therapeutic targeting of M1 receptors in various disease states in which M1 receptors are implicated (epilepsy, Parkinson′s disease, attention and cognitive disorders, dystonia, etc).

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