(R)-(+)-ALPHA-(2,3-DIMETHOXYPHENYL)-1-[2-(4-FLUORO-PHENYL)ETHYL]-4-PIPERIDINE METHANOL

Details:

Volinaserin is an effective and selective 5-HT2 receptor antagonist with a Ki value of 0.36 nM, and its selectivity is 300 times higher than that of 5-HT1c, alpha-1, and DA D2 receptors. It can be used for the study of mental disorders.
Related categories
Signal Pathways>>G Protein Coupled Receptors/G Proteins>>5-HT Receptors
Signal Pathways>>Neural Signal Pathways>>5-HT Receptors
Research Fields>>Neurological Diseases
Target point
Ki: 0.36 nM (5-HT2 receiver) [1]
In vitro studies have shown that Volinaserin (MDL 100907) is an effective antagonist of the 5-HT2 receptor, with a Ki of 0.36 nM, targeting the 5-HT1c receptor, α- The 5-HT2 receptor selectivity of DA D2 receptor and DA D2 receptor is 300 times. Volinaserin has antipsychotic activity [1].
In vivo studies showed that Volinaserin (MDL 100907; 0.008-2.0mg/kg, ip) significantly reduced d-phenylisopropylamine stimulated motor activity in mice, with an ED50 of 0.3mg/kg, but there was no significant decrease in baseline motor activity in mice. The ED50 of epileptic seizures produced by Volinaserin in rats is 10-50mg/kg. Volinaserin does not reduce apomorphine induced stereotyping or produce tonic syncope in rats [1]. The combination of Volinaserin (M100907) and MK-801 significantly reduces by 1 μ G/kg enhancer, but dose-dependent (10100 μ G/kg) antagonizes the destructive effect of MK-801 on rats through ip administration. Volinaserin (6.25 μ G/kg enhanced the antidepressant like effect of dexamethasone in the DRL 72-s schedule and increased the antidepressant like effect of anti phenylcyclopropamide [2].
In order to measure the effect of individual test compounds on spontaneous motor activity, animal experimental mice [1] were intraperitoneally injected with the test compound and placed separately in a transparent Plexiglas test cage (16 × sixteen × 8 inches) and adapt it to 30mm. For each of the six doses, six mice were tested for Volinaserin (0.008-2.0 mg/kg), ampicillin, and haloperidol per dose. Six doses of clozapine were tested in 12 mice per dose. In these experiments, 60 animal vectors were administered. Afterwards, place the box in the activity monitor and take a 30mm measurement. To measure the effects of various pre-treatments on amphetamine stimulated motor activity, mice (four per test box) were adapted to 90mm to reduce the spontaneous activity level of the control. Then, the mice were injected with amphetamine (2mg/kg ip) and the test compound, returned to the active box and tested for 90mm. Here