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

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

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

NCT00464061 / TerminatedPhase 3

Efficacy and Safety of 2mg/Day of M100907 on Sleep Maintenance Insomnia With a Sub-study of the Effect of M100907 on Stable Type II Diabetes Mellitus: a One Year, 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 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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472

Literatures (Medical) associated with Volinanserin

01 Dec 2024·Neuropharmacology

The psychedelic drug DOI reduces heroin motivation by targeting 5-HT2A receptors in a heroin and alcohol co-use model

Article

Author: Olson, David E ; Peters, Jamie ; Heinsbroek, Jasper A ; Kregar, Nathaniel P ; Heinsbroek, Jasper A. ; Bonilla, Joel ; Olson, David E. ; Giannotti, Giuseppe ; Kregar, Nathaniel P.

There has been a recent renewed interest in the potential use of psychedelic drugs as therapeutics for certain neuropsychiatric disorders, including substance use disorders. The psychedelic drug 2,5-dimethoxy-4-iodoamphetamine (DOI) has demonstrated therapeutic efficacy in preclinical models of opioid use disorder (OUD). Alcohol is commonly co-used in individuals with OUD, but preclinical models that recapitulate this comorbidity are lacking. We developed a polydrug model wherein male and female rats were allowed to self-administer intravenous heroin and oral alcohol (or saccharin control solution) over weeks of behavioral training, and then we conducted a series of progressive ratio tests to assess the animals' motivational state for heroin and alcohol. In this model, motivation for heroin is higher than alcohol, and DOI (0.4 mg/kg) administered prior to testing significantly reduced heroin motivation measured as the animals' break point, or maximum effort the animal is willing to expend to obtain a single infusion of heroin. The 5-HT2A receptor antagonist MDL 100,907 (0.3 mg/kg), but not the 5-HT2C receptor antagonist SB-242084 (0.5 mg/kg), blocked the therapeutic effect of DOI on heroin motivation. No significant effects on alcohol break points were observed, nor did MDL 100,907 or SB-242084 have any effect on break points on their own. These data support the view that psychedelic drugs like DOI may have therapeutic effects on opioid use in individuals with OUD and comorbid alcohol use, by acting as a 5-HT2A receptor agonist.

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.

01 Nov 2024·European Journal of Pharmacology

The serotonin(5-HT)2A receptor is involved in the hypersensitivity of bladder afferent neurons in cyclophosphamide-induced cystitis

Article

Author: Zhang, Lin ; Lv, Rong ; Gu, Baojun ; Li, Mingzhuo ; Cao, Nailong ; Sun, Yudong ; Chen, Xun

Interstitial cystitis/bladder pain syndrome (IC/BPS) is a chronic bladder inflammation characterized by the main symptoms of urinary frequency, urgency, and pelvic pain. The hypersensitivity of bladder afferent neurons is considered a significant pathophysiologic mechanism in IC/PBS. Serotonin (5-HT, 5-hydroxytryptamine) receptors are known to be involved in the regulation of the micturition reflex and hyperalgesia, but the effect of 5-HT receptors on cystitis remains unknown. In this study, a rat model of interstitial cystitis induced by intraperitoneal injection of cyclophosphamide (CYP) was used to investigate the role of 5-HT receptors on cystitis. The histology and urodynamics exhibited chronic cystitis and overactive bladder in CYP-treated rats. Notably, among 5-HT1A, 5-HT2A and 5-HT7 receptors, the expression of 5-HT2A receptor was significantly increased in bladder afferent neurons in CYP-treated rats. Intrathecal administration of the 5-HT2A receptor antagonist M100907 could alleviate bladder overactivity and hyperalgesia in CYP-induced cystitis rats. Neuronal calcium imaging of bladder afferent neurons revealed increased calcium influx induced by the 5-HT2A receptor agonist or capsaicin in cystitis rats, which could be inhibited by M100907. Moreover, RNA sequencing indicated that differentially expressed genes were enriched in inflammation-related pathways and cellular calcium homeostasis. These findings suggest that the 5-HT2A receptor is involved in the hypersensitivity of bladder afferent neurons in CYP-induced cystitis, and M100907 could alleviate bladder overactivity and hyperalgesia in CYP-induced cystitis by inhibiting neuronal hypersensitivity in the afferent pathways. The 5-HT2A receptor may be a potential therapeutic target for the treatment of IC/BPS.

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	BR	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	TR	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	AR	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	HK	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 3	BR	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 1	ZA	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Phase 1	AR	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Preclinical	HK	Sanofi	01 Apr 2007
Sleep Initiation and Maintenance Disorders	Preclinical	TR	Sanofi	01 Apr 2007