Drug intelligence / Profile preview

glemanserin

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

Glemanserin (MDL 11,939) is a selective, centrally active serotonin 5-HT2A receptor antagonist. Originally developed by Merrell Dow Pharmaceuticals (later Aventis, now Sanofi), glemanserin was the first highly selective 5-HT2A ligand discovered, serving as a precursor to the development of volinanserin (MDL-100,907). It was clinically evaluated up to Phase 3 trials for the treatment of generalized anxiety disorder and also investigated for cardiac arrhythmias, but development was discontinued due to lack of efficacy. In preclinical research, glemanserin is widely used as a tool compound to study the role of 5-HT2A receptors in memory retrieval, stress-induced anxiety, and opioid withdrawal.

Other names
(1-phenethylpiperidin-4-yl)(phenyl)methanolalpha-phenyl-1-(2-phenylethyl)-4-piperidine methanolalpha-phenyl-1-(2-phenylethyl)-4-piperidinemethanolglemanserin
02

Targets

HTR2A (Serotonin receptor 5-HT2A)

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