(R)-(+)-alpha-(2,3-Dimethoxyphenyl)-1-[2-(4-fluoro-phenyl)ethyl]-4-piperidine methanol

Description

Volinanserin is a potent and selective antagonist of the serotonin receptor 5-HT_2A (K_i = 0.36-0.85 nM). It weakly binds 5-HT_2C, α₁-adrenergic, and sigma receptors (K_i = 88, 128, and 87 nM) and much less effectively associates with other serotonin, dopamine, adrenergic, muscarinic acetylcholine receptors and monoamine transporters. Volinanserin displays antipsychotic activity, attenuates impulsivity, and augments antidepressant effects in vivo.

Chemical Properties

Colourless solid

Uses

Volinanserin is a serotonin receptor 5-HT2A antagonist; anti-psychotic.

Uses

As a serotonin 5-HT2A receptor antagonist, Volinanserin Hydrochloride Salt can be used as potential controls in various biological studies.

General Description

M100907 blocks the serotonin 2A (5-HT2A) receptors and imposes antidepressant-like effects. It may be used for treating dopaminergic anomalies.

Biochem/physiol Actions

M100907 is a selective 5-HT2A Antagonist.

storage

+4°C

References

[1] S M SORENSEN. Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: behavioral, electrophysiological and neurochemical studies.[J]. Journal of Pharmacology and Experimental Therapeutics, 1993, 266 2: 684-691.
[2] J H KEHNE. Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile.[J]. Journal of Pharmacology and Experimental Therapeutics, 1996, 277 2: 968-981.
[3] ELIZABETH A PEHEK. Evidence for the Preferential Involvement of 5-HT2A Serotonin Receptors in Stress- and Drug-Induced Dopamine Release in the Rat Medial Prefrontal Cortex[J]. Neuropsychopharmacology, 2005, 31 2: 265-277. DOI: 10.1038/sj.npp.1300819
[4] PAUL A ARDAYFIO. The 5-hydroxytryptamine2A receptor antagonist R-(+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl-4-piperidinemethanol (M100907) attenuates impulsivity after both drug-induced disruption (dizocilpine) and enhancement (antidepressant drugs) of differential-reinforcement-of-low-rate 72-s behavior in the rat.[J]. Journal of Pharmacology and Experimental Therapeutics, 2008, 327 3: 891-897. DOI: 10.1124/jpet.108.143370
[5] LAURA J. BOOTHMAN  Trevor S  Stephen N Mitchell. Investigation of the SSRI augmentation properties of 5-HT2 receptor antagonists using in vivo microdialysis[J]. Neuropharmacology, 2006, 50 6: Pages 726-732. DOI: 10.1016/j.neuropharm.2005.11.020
[6] VERN LEWIS. A non-hallucinogenic LSD analog with therapeutic potential for mood disorders.[J]. Cell reports, 2023, 42 3: 112203. DOI: 10.1016/j.celrep.2023.112203