[CAS NO. 139290-65-6] Volinanserin

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PRODUCTS SPECIFICATIONS [139290-65-6]

Catalog

HY-14940

Brand

MCE

CAS

139290-65-6

DESCRIPTION [139290-65-6]

Overview

MDL	MFCD00909060
Molecular Weight	373.46
Molecular Formula	C22H28FNO3
SMILES	FC1=CC=C(CCN2CCC([C@@]([H])(O)C3=CC=CC(OC)=C3OC)CC2)C=C1

For research use only. We do not sell to patients.

3 Publications Citing Use of MCE

Summary

Volinanserin is a potent and selective antagonist of 5-HT ₂ receptor , with a K _i of 0.36 nM, and shows 300-fold selectivity for 5-HT ₂ receptor over 5-HT _1c , alpha-1 and DA D ₂ receptors. Volinanserin has antipsychotic activity.

IC50 & Target

5-HT ₂ Receptor

0.36 nM (Ki)

In Vitro

Volinanserin (MDL 100907) is a potent antagonist at the 5-HT ₂ receptor, with a K _i of 0.36 nM, and shows 300-fold selectivity for 5-HT ₂ receptor over 5-HT _1c receptor, alpha-1 and DA D ₂ receptors. Volinanserin has antipsychotic activity ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Volinanserin (MDL 100907; 0.008-2.0 mg/kg, i.p.) significantly decreases d-amphetamine-stimulated locomotor activity in mice, with an ED ₅₀ of 0.3 mg/kg, but shows no obvious reduction in the base-line locomotor activity in mice. Volinanserin produces atalepsy with an ED ₅₀ of 10-50 mg/kg in rats. Volinanserin does not reduces apomorphine-induced stereotypies or produces catalepsy in rats ^[1] . Volinanserin (M100907) combined with MK-801 significantly decreases reinforcers at 1 μg/kg, but dose-dependently (10, 100 μg/kg) antagonizes the disruptive effect of MK-801 in rats via i.p. administration. Volinanserin (6.25 μg/kg) enhances the antidepressant-like action of desipramine in rats performing under a DRL 72-s schedule, and elevates the antidepressant-like effect of tranylcypromine ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00464243	Sanofi	Sleep Initiation and Maintenance Disorders	April 2007	Phase 3
NCT00464061	Sanofi	Sleep Initiation and Maintenance Disorders	April 2007	Phase 3
NCT00788515	Sanofi	Sleep Initiation and Maintenance Disorders	November 2008	Phase 3
NCT00495885	Sanofi	Sleep Initiation and Maintenance Disorders	June 2007	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 133.88 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6777 mL	13.3883 mL	26.7766 mL
5 mM	0.5355 mL	2.6777 mL	5.3553 mL
10 mM	0.2678 mL	1.3388 mL	2.6777 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

4-Piperidinemethanol, α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-, (αR)-

4-Piperidinemethanol, α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-, (R)-

(αR)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol

MDL 100907

(+)-α-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol

M 100907

(+)-MDL 100907

R-MDL 100907

Volinanserin

(R)-(2,3-Dimethoxyphenyl)-[1-[2-(4-fluorophenyl)ethyl]piperidin-4-yl]methanol