5-HT6/7 antagonist 1

5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

5-HT6/7/2A, D2[1]

Targeting 5-HT6 and/ or 5-HT7 receptors with antagonist drugs could constitute a promising strategy for treating symptoms of BPSD while avoiding some of the side effects of current antipsychotic drugs. Nevertheless, due to the complex pathology of dementia and accompanying behavioral and psychological symptoms, it seems unlikely that focusing on a single therapeutic target would be sufficient to provide adequate clinical benefit, and it is likely that successful development of novel anti-BPSD agents should involve a “designed” multifactorial approach[1].

[1]. Kołaczkowski M, et al. Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia. J Med Chem. 2014 Jun 12;57(11):4543-57.

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