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    WAY-100635 Maleate
    WAY-100635 Maleate

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0996
    CAS #: 1092679-51-0 or 634908-75-1Purity ≥98%

    Description: WAY-100635 maleate (WAY 100635; WAY100635), the maleate salt of WAY-100635, is a novel, potent and selective antagonist of serotonin 5-HT1A receptor with important biological activity. It inhibits 5-HT1A receptor with IC50 of 0.95 nM.  

    References: J Pharmacol Exp Ther. 1996 Aug;278(2):679-88; Behav Brain Res. 1996;73(1-2):337-53.

    Related CAS#:162760-96-5 (WAY 100635 free); 634908-75-1 (WAY-100635 maleate)

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    Molecular Weight (MW)538.64 
    CAS No.1092679-51-0 (WAY-100635 maleate)
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (157.8 mM) 
    Water: <1 mg/mL
    Ethanol: 85 mg/mL (157.8 mM) 
    Other infoChemical Name: N-(2-(4-(2-Methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide Maleate
    InChi Code: InChI=1S/C25H34N4O2.C4H4O4/c1-31-23-12-6-5-11-22(23)28-18-15-27(16-19-28)17-20-29(24-13-7-8-14-26-24)25(30)21-9-3-2-4-10-21;5-3(6)1-2-4(7)8/h5-8,11-14,21H,2-4,9-10,15-20H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
    SynonymsWAY 100635 Maleate; WAY-100635; WAY100635

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    In Vitro

    In vitro activity: In dorsal raphe nucleus (DRN) slices superfused with WAY 100635 (10 nM), the majority of putative 5-HT neurons increase their firing rate (13% of baseline rate). In addition, WAY 100635 completely prevents the decrease in firing rate produced by 5-HT (3-15 μM), 8-OH-DPAT (10 nM), 5-carboxamidotryptamine (20 nM) and lesopitron (100 nM). The antagonism exerted by WAY 100635 is fully surmounted by increasing the concentration of 5-HT to 300 μM with an IC50 of 0.95 nM. In hippocampal slices, WAY 100635 (0.5 nM -10 nM) does not alter the resting membrane potential or the membrane input resistance of intracellularly recorded CA1 pyramidal cells. However, WAY 100635 completely prevents not only the hyperpolarization, with an IC50 of 1.3 nM, but also the decrease in membrane input resistance produced by 5-HT and 5-carboxamidotryptamine with IC50 of 22.5 μM and 50 nM, respectively. WAY 100635 has an IC50 of 1.35 nM and is > 100-fold selective for the 5-HT1A site relative to a range of other CNS receptors. The Bmax of [3H]WAY 100635 specific binding is consistently 50-60% greater than that of the agonist radioligand, [3H]8-OH-DPAT. Mn2+, but not guanine nucleotides, inhibits [3H]WAY 100635-specific binding. WAY 100635 has no 5-HT1A receptor agonist actions, but dose-dependently blocks the effects of agonists at both the postsynaptic 5-HT1A receptor in the CA1 region of the hippocampus, and the somatodendritic 5-HT1A receptor locates on dorsal raphe 5-HT neurones. [3H]WAY 100635 has a Kd of approximately 2.5 nM. In the isolated guinea-pig ileum WAY 100635 is a potent and, at high concentrations, an insurmountable antagonist of the 5-HT1A receptor agonist action of 5-carboxamidotryptamine, with an apparent pA2 value (at 0.3 nM) of 9.71.

    Cell Assay: 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.

    In Vivo[3H]WAY 100635 is shown to bind selectively to brain 5-HT1A receptors, following intravenous administration to mice. WAY 100635 also dose-dependently blocks the ability of 8-OH-DPAT to inhibit the firing of dorsal raphe 5-HT neurones, and to induce the '5-HT syndrome', hypothermia, hyperphagia and to elevate plasma ACTH levels. In the mouse light/dark box anxiety model, WAY 100635 induces anxiolytic-like effects. WAY 100635 has no intrinsic effect on cognition in the delayed-matching-to-position model of short-term memory in the rat, but reverses the disruptive effects of 8-OH-DPAT on motor motivational performance. WAY 100635 blocks the inhibitory action of 8-OH-DPAT on dorsal raphe neuronal firing in the anaesthetised rat at doses which has no inhibitory action per se. In behavioural models, WAY 100635 itself induces no overt behavioural changes but potently antagonises the behavioural syndrome induced by 8-OH-DPAT in the rat and guinea-pig (minimum effective dose = 0.003 mg/kg s.c. and ID50 = 0.01 mg/kg s.c., respectively). WAY 100635 also blocks the hypothermia induced by 8-OH-DPAT in the mouse and rat with ID50 values of 0.01 mg/kg s.c. 
    Animal modelMale CD1 mice with 25-30 g body weight 
    Formulation & DosageDissolved in  0.9% NaCl; 250 μL (30.4 μCi/mL); i.v. injection 
    ReferencesJ Pharmacol Exp Ther. 1996 Aug;278(2):679-88; Behav Brain Res. 1996;73(1-2):337-53. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    WAY-100635 Maleate
    Effect of the 5-HT1A Antagonist WAY 100635 on the Activity of PG01042, PG01037 and Buspirone. Neuropharmacology. 2009 May-Jun; 56(0): 10.1016/j.neuropharm.2009.01.020.
    WAY-100635 Maleate
    Effect of the 5-HT1A antagonist WAY 100635 on the activity of PG01037. Neuropharmacology. 2009 May-Jun; 56(0): 10.1016/j.neuropharm.2009.01.020.
    WAY-100635 Maleate
    Effects of WAY-100635 treatment on cytokine release into CSF, NLRP3 expression and signaling pathways activation in hippocampus and BLA. BMC Neurosci. 2016; 17: 66.


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