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Volinanserin

Catalog No. T5389   CAS 139290-65-6
Synonyms: M 100907, MDL100907

Volinanserin (MDL100907) (MDL 100907) is a potent and selective antagonist of the serotonin receptor 5-HT2 (Ki: 0.36 nM) and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 adrenergic and sigma receptors.

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Volinanserin Chemical Structure
Volinanserin, CAS 139290-65-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 82.00
10 mg In stock $ 127.00
25 mg In stock $ 246.00
50 mg In stock $ 317.00
200 mg In stock $ 694.00
1 mL * 10 mM (in DMSO) In stock $ 88.00
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Purity: 99.95%
Purity: 99.23%
Purity: 98.94%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Volinanserin (MDL100907) (MDL 100907) is a potent and selective antagonist of the serotonin receptor 5-HT2 (Ki: 0.36 nM) and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 adrenergic and sigma receptors.
Targets&IC50 5-HT2 receptor:0.36 nM (Ki)
In vitro MDL 100,907 demonstrated low nanomolar or subnanomolar binding in vitro at the 5-HT2A receptor and showed a > 100-fold separation from all other receptors measured. MDL 100,907 had subnanomolar potency as a 5-HT2A antagonist in vitro in reversing 5-HT-stimulated inositol phosphate accumulation in NIH 3T3 cells transfected with the rat 5-HT2A receptor [2].
In vivo In mice, MDL 100,907 blocked amphetamine-stimulated locomotion at doses that did not significantly affect apomorphine-stimulated climbing behavior. When administered chronically, MDL 100,907 selectively reduced the number of spontaneously active A10 neurons [1]. In vivo, MDL 100,907 potently inhibited 5-methoxy-N, N-dimethyltryptamine-induced head twitches in mice or 5-hydroxytryptophan-induced head twitches in rats. In vivo, functional tests in mice revealed a > 500-fold separation between doses that produced 5-HT2A antagonism and doses that produced alpha 1-adrenergic or striatal D2 antagonism [2].
Synonyms M 100907, MDL100907
Molecular Weight 373.46
Formula C22H28FNO3
CAS No. 139290-65-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (267.8 mM)

Ethanol: 18 mg/mL (48.2 mM)

TargetMolReferences and Literature

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. 2. Kehne JH, et al. Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile. J Pharmacol Exp Ther. 1996 May;277(2):968-81.

TargetMolCitations

1. Zhu H, Liu X, Wang X, et al.Gβγ subunit inhibitor decreases DOM-induced head twitch response via the PLCβ/IP3/Ca2+/ERK and cAMP signaling pathways.European Journal of Pharmacology.2023: 176038. 2. Gao H, Liu X, Xie L, et al.Modulation of DOM-Induced Head-Twitch Response by mGluR2 Agonist/Inverse Agonist is Associated with 5-HT2AR-Mediated Gs Signaling Pathway.Neurochemical Research.2023: 1-13.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library GPCR Compound Library Anti-Cancer Clinical Compound Library Anti-Parkinson's Disease Compound Library Bioactive Compound Library Angiogenesis related Compound Library

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Keywords

Volinanserin 139290-65-6 GPCR/G Protein Neuroscience 5-HT Receptor M100907 M 100907 Serotonin Receptor inhibit MDL100907 5-hydroxytryptamine Receptor Inhibitor MDL-100907 M-100907 MDL 100907 inhibitor

 

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