(-)-MDL 100907
(-)-MDL 100907 Basic information
- Product Name:
- (-)-MDL 100907
- Synonyms:
-
- (S)-(2,3-DIMETHOXY-PHENYL)-(1-[2-(4-FLUORO-PHENYL)-ETHYL]-PIPERIDIN-4-YL)-METHANOL
- (S)-MDL 100907
- 4-PIPERIDINEMETHANOL, A-(2,3-DIMETHOXYPHENYL)-1-[2-(4-FLUOROPHENYL)ETHYL]-, (AS)-
- M 100009
- MDL 100009
- MDL 100009 - MDL 100907, (S)-(-)-
- 4-Piperidinemethanol, α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-, (αS)-
- (S)-(2,3-Dimethoxyphenyl)(1-(4-fluorophenethyl)piperidin-4-yl)methanol
- CAS:
- 175673-57-1
- MF:
- C22H28FNO3
- MW:
- 373.465
- Product Categories:
-
- Selective 5-HT2A antagonist.
- Mol File:
- 175673-57-1.mol
(-)-MDL 100907 Chemical Properties
- Boiling point:
- 499.4±45.0 °C(Predicted)
- Density
- 1.150±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Ethanol: Soluble: =10 mg/ml
- pka
- 13.93±0.20(Predicted)
(-)-MDL 100907 Usage And Synthesis
Uses
(S)-Volinanserin is an isform of Volinanserin (HY-14940). Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
in vivo
Volinanserin (MDL 100907; 0.008-2.0 mg/kg, i.p.) significantly decreases d-amphetamine-stimulated locomotor activity in mice, with an ED50 of 0.3 mg/kg, but shows no obvious reduction in the base-line locomotor activity in mice. Volinanserin produces atalepsy with an ED50 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 (HY-B1272A) in rats performing under a DRL 72-s schedule, and elevates the antidepressant-like effect of Tranylcypromine (HY-17447)[2].
References
[1] Sorensen SM, 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. 1993 Aug;266(2):684-91. PMID:8102646
[2] Ardayfio PA, et al. 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 Pharmacol Exp Ther. 2008 Dec;327(3):891-7. DOI:10.1124/jpet.108.143370
[3] TIMO HEINRICH DR. 1-(1-Phenethylpiperidin-4-yl)-1-phenylethanols as Potent and Highly Selective 5-HT2A Antagonists[J]. ChemMedChem, 2006, 1 2: 245-255. DOI: 10.1002/cmdc.200500023
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