WAY-100635 Monomaleate

SKU: orb1305242

Description

WAY-100635 maleate is a potent and selective 5-HT1A receptor antagonist (IC50 0.91 nM) with additional activity as a dopamine D4 agonist and α1-adrenergic binding. It is widely used in neuroscience research to investigate serotonin and dopamine systems in both in vitro and in vivo experimental models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1092679-51-0
MW	538.64
Purity	>99.99% (May vary between batches)
Formula	C₂₅H₃₄N₄O₂·C₄H₄O₄
SMILES	OC(=O)\C=C/C(O)=O.COc1ccccc1N1CCN(CCN(C(=O)C2CCCCC2)c2ccccn2)CC1
Target	5-HT Receptor,Dopamine Receptor
Solubility	Ethanol:79 mg/mL (146.67 mM);DMSO:55 mg/mL (102.11 mM)

Bioactivity

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Target IC50	sPLA2:9.71 (pA2)\|sPLA2:8.87 (pIC50)\|5-HT:0.95 nM
In Vivo	The antagonistic effect produced by WAY 100635 was mediated by increasing the concentration of 5-HT to 300 μM with an IC50 of 0.95 nM.
In Vitro	The antagonistic effect produced by WAY 100635 was mediated by increasing the concentration of 5-HT to 300 μM with an IC50 of 0.95 nM.
Cell Research	Extracellular recordings are made with glass microelectrodes filled with 2 M NaC1 (12 MΩ-15 MΩ). Cells are identified as 5-HT neurons according to the following criteria: biphasic action potentials of 2 msec to 3 msec in duration, slow (0.5 Hz - 2.0 Hz) and regular pattern of discharge. Firing is evoked in the otherwise silent neurons by adding the alpha-l adrenergic agonist phenylephrine (3 μM) to the superfusing ACSF. Baseline activity is recorded for at least 10 minutes before application of the different drugs. The electric signals are fed into a high-input impedance amplifier, an oscilloscope and an electronic ratemeter triggered by individual action potentials connected to an A/D converter and a personal computer. Using dedicated software, the integrated firing rate is recorded, computed and displayed on a chart recorder as consecutive 10-sec samples. The effects of agonists are evaluated by comparing the mean discharge frequency recorded during the 2 minutes that preceded WAY 100635 application with that recorded at the peak of WAY 100635 action (usually 2-5 minutes after the beginning of application). When the agonists are applied in the presence of the antagonist, the effect of the agonist is compared to baseline firing rate and to the frequency recorded during superfusion of the antagonist alone. The antagonist is left to equilibrate for 10 minutes to 25 minutes before retesting of the action of agonists. (Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Dopamine Receptor, Dopamine, DopamineReceptor, 5-HT, 5HT Receptor, 5-hydroxytryptamine Receptor, 5HTReceptor, 5-HT Receptor, inhibit, Inhibitor, Serotonin Receptor, WAY-100635 Maleate, WAY100635, WAY-100635, WAY100635 Maleate, WAY 100635, WAY 100635 Maleate

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Compound Identifiers

PubChem CID

11957721 ↗

Key Properties

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No computed properties available.

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