Delving into the Latest Updates on Volinanserin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [5]

Target

5-HT2 receptor x 5-HT2A receptor

Action

antagonists

Mechanism

5-HT2 receptor antagonists(Serotonin 2 (5-HT2) receptor antagonists), 5-HT2A receptor antagonists(Serotonin 2a (5-HT2a) receptor antagonists)

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Diabetes Mellitus, Type 2Sleep Initiation and Maintenance Disorders

Originator Organization

Sanofi

Active Organization-

Inactive Organization

Sanofi

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC22H28FNO3

InChIKeyHXTGXYRHXAGCFP-OAQYLSRUSA-N

CAS Registry139290-65-6

The primary objective is to compare the potential for next-day residual effects of volinanserin 2 mg/day and lormetazepam 1 mg/day by measuring the sleepiness in the morning using the patient's sleep questionnaire during 4 weeks of treatment in patients with chronic primary insomnia and sleep maintenance difficulties.
Secondary objectives are to compare the clinical safety of both products, including the potential for rebound insomnia and withdrawal symptoms after treatment discontinuation, to compare the efficacy of both products on subjective sleep parameters and to compare the effects of both products on patient's daytime functioning.

Start Date01 Nov 2008

Sponsor / Collaborator

Sanofi

NCT00495885

/ CompletedPhase 3

Efficacy and Safety of 2 mg/Day of M100907 on Sleep Maintenance Insomnia With a Sub-study of the Effect of M100907 on Stable Type II Diabetes Mellitus: a 12-week, Multi-center, Randomized, Double-blind, Placebo-controlled Study

The purpose of this study is to assess efficacy and safety of volinanserin in the population of patients complaining of sleep maintenance insomnia. The objective of the substudy is to assess glycemic control in the subgroup of patients with type II diabetes mellitus.

Start Date01 Jun 2007

Sponsor / Collaborator

Sanofi

NCT00464243

/ CompletedPhase 3

Efficacy and Safety of 2 mg/Day M100907 on Sleep Maintenance Insomnia: a 6-week, Multicenter, Randomized, Double-blind, Placebo-controlled Polysomnographic Study

The purpose of this study is to assess efficacy and safety of volinanserin in the population of patients complaining of sleep maintenance insomnia. The patients suffering from that condition frequently wake up during the night, their sleep is non restorative and they suffer from a significant distress or impairment in their daily activities consecutive to insomnia.

Start Date01 Apr 2007

Sponsor / Collaborator

Sanofi

100 Clinical Results associated with Volinanserin

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100 Translational Medicine associated with Volinanserin

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100 Patents (Medical) associated with Volinanserin

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596

Literatures (Medical) associated with Volinanserin

01 Feb 2025·Journal of Cerebral Blood Flow & Metabolism

Imaging the 5-HT_2C receptor with PET: Evaluation of 5-HT_2C and 5-HT_2A affinity of pimavanserin in the primate brain

Article

Author: Stepanov, Vladimir ; Forsberg Morén, Anton ; Rabiner, Eugenii A ; Ridler, Khanum ; Rizzo, Gaia ; Halldin, Christer ; Burstein, Ethan S

Two complimentary techniques were used to estimate occupancy of pimavanserin (a selective 5-HT2A/2C inverse agonist) to 5-HT2A and 5-HT2C receptors in non-human primate brains. One employed the 5-HT2A/2C selective radioligand [11C]CIMBI-36 combined with quantification of binding potentials in brain regions known to be enriched in 5-HT2A (cortex) or 5-HT2C (choroid plexus) receptors to estimate occupancy. Pimavanserin was 6–10 fold more potent displacing [11C]CIMBI-36 from cortex (ED50 = 0.007 mg/kg; EC50 = 0.6 ng/ml) than from choroid plexus (ED50 =0.046 mg/kg; EC50 = 6.0 ng/ml). The assignment of [11C]CIMBI-36 binding to 5-HT2A and 5-HT2C receptors by anatomical brain structure was confirmed using the 5-HT2A selective inverse agonist MDL 100,907 and the 5-HT2C selective antagonist SB 242584 to displace [11C]CIMBI-36. The second technique employed a novel, 5-HT2C selective tracer called [11C]AC1332. [11C]AC1332 bound robustly to choroid plexus, moderately to hippocampus, and minimally to cortex. Pimavanserin displaced [11C]AC1332 with similar potency (ED50 = 0.062 mg/kg; EC50 = 2.5 ng/ml) as its potency displacing [11C]CIMBI-36 binding from choroid plexus. These results demonstrate the feasibility of simultaneously estimating drug occupancy of 5-HT2A and 5-HT2C receptors in vivo, and the utility of a novel 5-HT2C receptor selective tracer ligand.

01 Jan 2025·Progress in Neuro-Psychopharmacology and Biological Psychiatry

The psychoplastogens ibogaminalog and ibogainalog induce antidepressant-like activity in naïve and depressed mice by mechanisms involving 5-HT2A receptor activation and serotonergic transmission

Article

Author: Manetti, Dina ; Romanelli, Maria Novella ; Valenta, Jan ; Olejarz-Maciej, Agnieszka ; Rudin, Deborah ; De Deurwaerdère, Philippe ; Czartoryska, Zofia ; Handzlik, Jadwiga ; Doroz-Płonka, Agata ; Chagraoui, Abdeslam ; Arias, Hugo R ; Leśniak, Anna ; Luethi, Dino ; Liechti, Matthias E

The antidepressant-like activity of two psychoplastogens, ibogainalog (IBG) and ibogaminalog (DM506), was studied in naïve mice using the forced swim test (FST) and tail suspension test (TST). The behavioral results showed that a single administration of 25 mg/kg DM506 or 10 mg/kg IBG induced antidepressant-like activity in naïve mice in a volinanserin-sensitive manner that persisted for 72 h. Similar results were observed using the chronic immobilization stress (CIS) test, in which depression symptoms were reduced for 48 h. To assess the contribution of serotonergic and/or norepinephrinergic neurotransmission, serotonin (5-HT) and norepinephrine (NE) levels were depleted. The reduction in 5-HT levels, but not NE levels, inhibited the antidepressant-like activity of ibogalogs, suggesting that serotonergic transmission may play a more significant role than norepinephrinergic transmission. Concurrently, DM506, IBG, and TBG (derived from tabernanthine) inhibited monoamine transporters with the following order of selectivity: SERT > NE transporter > dopamine transporter. The IBG exhibited the highest selectivity for SERT. Only TBG inhibited monoamine oxidase A activity, indicating its relatively minor role. Radioligand and functional assays showed that all ibogalogs bind to the 5-HT₂ receptor subfamily (DM506 > IBG > TBG) and fully activate 5-HT_2A/2C receptors with similar potency in the nM range. However, they act as competitive antagonists of the 5-HT_2B receptor, with DM506 as an exception, exhibiting partial but potent agonist activity. In conclusion, ibogalogs induce acute and sustained antidepressant-like activity in naïve and depressed mice through mechanisms involving 5-HT_2A receptor activation and serotonergic transmission.

01 Dec 2024·Neuropharmacology

Activation of ventral pallidum-projecting neurons in the nucleus accumbens via 5-HT2C receptor stimulation regulates motivation for wheel running in male mice

Article

Author: Nishitani, Naoya ; Futami, Yusaku ; Kaneda, Katsuyuki ; Deyama, Satoshi ; Nishida, Ryoma ; Niitani, Kazuhei

Rodents have a strong motivation for wheel running; however, the neural mechanisms that regulate their motivation remain unknown. We investigated the possible involvement of serotonin (5-HT) systems in regulating motivation for wheel running in male mice. Systemic administration of a 5-HT_1A receptor antagonist (WAY100635) increased the number of wheel rotations, whereas administration of a 5-HT_2A or 5-HT_2C receptor antagonist (volinanserin or SB242084, respectively) decreased it. In the open field test, neither WAY100635 nor volinanserin affected locomotor activity, whereas SB242084 increased locomotor activity. To identify the brain regions on which these antagonists act, we locally injected these into the motivational circuitry, including the nucleus accumbens (NAc), dorsomedial striatum (DM-Str), and medial prefrontal cortex (mPFC). Injection of SB242084 into the NAc, but not the DM-Str or mPFC, reduced the number of wheel rotations without altering locomotor activity. The local administration of WAY100635 or volinanserin to these brain regions did not affect the number of wheel rotations. Immunohistochemical analyses revealed that wheel running increased the number of c-Fos-positive cells in the NAc medial shell (NAc-MS), which was reduced by systemic SB242084 administration. In vitro slice whole-cell recordings showed that bath application of the 5-HT_2C receptor agonist lorcaserin increased the frequency of spontaneous excitatory and inhibitory postsynaptic currents in the ventral tegmental area (VTA)-projecting neurons, whereas it only increased the frequency of spontaneous excitatory postsynaptic currents in ventral pallidum (VP)-projecting neurons in the NAc-MS. These findings suggest that the activation of VP-projecting NAc-MS neurons via 5-HT_2C receptor stimulation regulates motivation for wheel running.

100 Deals associated with Volinanserin

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Volinanserin	-	DB16351

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Sleep Initiation and Maintenance Disorders	Phase 3	Italy	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Italy	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	United States	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Chile	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Chile	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Canada	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	United States	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Canada	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Singapore	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	Singapore	Sanofi	01 Apr 2007