WAY-100635 Maleate
For research use only.
Catalog No.S2663
6 publications
CAS No. 1092679-51-0
WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.
2 Customer Reviews
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Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P , 0.05 as compared to vehicle control group (N=8 per group). The 5-HT1A receptor antagonist WAY100635 does not block the antinociceptive effects of 40 mg/kg sinomenine.
Sci Rep, 2014, 4:7270.. WAY-100635 Maleate purchased from Selleck.
The effects of D1 antagonist Sch23390 and 5-HT1A antagonist WAY-100635 on CK’s antidepressant behavioral effects. Sch23390 (0.05 mg/kg) or WAY-100635 (0.2 mg/kg) was administered (s.c.) 30 min before CK once daily for consecutive 14 days, and TST (a) was performed on day 13, FST (b) on day 14. For CUMS model study, after 2 weeks of CUMS, the antagonists were administrated respectively for 4 weeks, and then sucrose preference (c) and open field test (d) were performed. FST chronic forced swimming test, TST tail suspension test. Data represent means ± SEM (n = 12/group). *p < 0.05, **p < 0.01, one-way ANOVA with post-hoc Tukey’s HSD test or Dunnett’s t test; #p < 0.05, two-way repeated-measures ANOVA interaction.
Neurochem Res, 2018, 43(7):1371-1382. WAY-100635 Maleate purchased from Selleck.
Purity & Quality Control
Choose Selective 5-HT Receptor Inhibitors
Biological Activity
| Description | WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM. | ||
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| Features | Characterised as the first 5-HT1A antagonist radioligand. | ||
| Targets |
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| In vitro |
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. [1] 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. [2] [3H]WAY 100635 has a Kd of approximately 2.5 nM. [3] 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. [4] Five minutes after the i.v. injection of [3H]WAY 100635 (4 μCi -7.6 μCi per mouse) the amount of tritium found in the whole brain only accounted for 1.5-1.8% of the injected radioactivity, regional differences in 3H accumulation already correspondes to those of 5-HT1A receptor density. [5] In light of its only recently discovered dopaminergic activity, conclusions drawn from studies that employs WAY 100635 as a selective 5-HT1A antagonist may need to be re-evaluated. [6] |
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| 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. [2] 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. [4] |
Protocol
| Cell Research: |
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Solubility (25°C)
| In vitro | DMSO | 85 mg/mL (157.8 mM) |
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| Ethanol | 85 mg/mL (157.8 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+40% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing. |
10mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 538.64 |
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| Formula | C25H34N4O2.C4H4O4 |
| CAS No. | 1092679-51-0 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.C(=CC(=O)O)C(=O)O |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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