Selective antagonist of the serotonin receptor 5-HT2A
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Enantiomer(s)
42955(−)-Volinanserin
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Volinanserin

Item No. 15936

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αR-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol
CAS Number
139290-65-6
Synonyms
  • MDL 100907
  • M100907
Molecular Formula
C22H28FNO3
Formula Weight
373.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 15 mg/mlEthanol: 20 mg/ml
SMILES
FC1=CC=C(CCN2CCC([C@@H](O)C3=CC=CC(OC)=C3OC)CC2)C=C1
InChi Code
InChI=1S/C22H28FNO3/c1-26-20-5-3-4-19(22(20)27-2)21(25)17-11-14-24(15-12-17)13-10-16-6-8-18(23)9-7-16/h3-9,17,21,25H,10-15H2,1-2H3/t21-/m1/s1
InChi Key
HXTGXYRHXAGCFP-OAQYLSRUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    Product Description

    Volinanserin is a potent and selective antagonist of the serotonin receptor 5-HT2A (Ki = 0.36-0.85 nM).1,2 It weakly binds 5-HT2C, α1-adrenergic, and sigma receptors (Ki = 88, 128, and 87 nM) and much less effectively associates with other serotonin, dopamine, adrenergic, muscarinic acetylcholine receptors and monoamine transporters.2,3 Volinanserin displays antipsychotic activity, attenuates impulsivity, and augments antidepressant effects in vivo.1,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sorensen, S.M., Kehne, J.H., Fadayel, G.M., et al. Characterization of the 5-HT2 receptor antagonist MDL 100907 as a putative atypical antipsychotic: Behavioral, electrophysiological and neurochemical studies. J. Pharmacol. Exp. Ther. 266(2), 684-691 (1993).

    2. Kehne, J.H., Baron, B.M., Carr, A.A., et al. 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. Pharmacol. Exp. Ther. 277(2), 968-981 (1996).

    3. Pehek, E.A., Nocjar, C., Roth, B.L., et al. Evidence for the preferential involvement of 5-HT2A serotonin receptors in stress- and drug-induced dopamine release in the rat medial prefrontal cortex. Neuropsychopharmacology 31(2), 265-277 (2006).

    4. Ardayfio, P.A., Benvenga, M.J., Chaney, S.F., et al. The 5-hydroxytryptamine2A receptor antagonist R-(+)-α-(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. Pharmacol. Exp. Ther. 327(3), 891-897 (2008).

    5. Boothman, L.J., Mitchell, S.N., and Sharp, T. Investigation of the SSRI augmentation properties of 5-HT2 receptor antagonists using in vivo microdialysis. Neuropharmacology 50(6), 726-732 (2006).

    Product Citations

    Lewis, V., Bonniwell, E.M., Lanham, J.K., et al. A non-hallucinogenic LSD analog with therapeutic potential for mood disorders. Cell Rep. 42(3), 112203 (2023).