WAY-100635 Maleate

Alias: WAY 100635 Maleate; WAY-100635; WAY100635
Cat No.:V0996 Purity: ≥98%
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.
WAY-100635 Maleate Chemical Structure CAS No.: 1092679-51-0
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of WAY-100635 Maleate:

  • WAY 100635
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Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
Targets
D4 Receptor; sPLA2 ( pIC50 = 8.87 ); sPLA2 ( pA2 = 9.71 )
ln Vitro

In vitro activity: WAY 100635 (10 nM) superfused dorsal raphe nucleus (DRN) slices causes most putative 5-HT neurons to fire at a rate of 13% above baseline. Moreover, 5-HT (3–15 μM), 8–OH–DPAT (10 nM), 5-carboxamidotryptamine (20 nM), and lesopitron (100 nM) all totally inhibit the reduction in firing rate that WAY 100635 causes. Increasing the concentration of 5-HT to 300 μM with an IC50 of 0.95 nM completely overcomes the antagonistic effect of WAY 100635. The membrane input resistance and resting membrane potential of intracellularly recorded CA1 pyramidal cells in hippocampal slices are not affected by WAY 100635 (0.5 nM–10 nM). WAY 100635, on the other hand, completely blocks both the hyperpolarization (IC50 = 1.3 nM) and the membrane input resistance decrease caused by 5-HT and 5-carboxamidotryptamine (IC50 = 22.5 μM and 50 nM, respectively).[1] WAY 100635 is > 100-fold selective for the 5-HT1A site in comparison to a variety of other CNS receptors, with an IC50 of 1.35 nM. Mn2+ can inhibit [3H]WAY 100635-specific binding, but not guanine nucleotides. The Bmax of [3H]WAY 100635 specific binding is consistently 50–60% greater than that of the agonist radioligand, [3H]8–OH-DPAT. Way 100635 does not act as a 5-HT1A receptor agonist; however, it dose-dependently inhibits the effects of agonists at the dorsal raphe 5-HT neurone and the postsynaptic 5-HT1A receptor in the CA1 region of the hippocampus. **[2]** [3H]. Its Kd is roughly 2.5 nM for WAY 100635.[3] At 0.3 nM, WAY 100635 exhibits an apparent pA2 value of 9.71, indicating its potency and insurmountable nature as a 5-HT1A receptor agonist in the isolated guinea-pig ileum.[4] The amount of tritium found in the entire brain only accounted for 1.5–1.8% of the injected radioactivity five minutes after the intravenous injection of [3H]WAY 100635 (4 μCi–7.6 μCi per mouse). Regional differences in 3H accumulation already correspond to those of 5-HT1A receptor density.[5] Conclusions from studies using WAY 100635 as a selective 5-HT1A antagonist may need to be reevaluated in light of its recently discovered dopaminergic activity.[6]

ln Vivo
[3H]WAY 100635 is demonstrated to bind specifically to 5-HT1A receptors in the brain after being given intravenously to mice. Additionally, WAY 100635 dose-dependently inhibits 8-OH-DPAT'scapacityto cause the "5-HT syndrome," hypothermia, hyperphagia, and an increase in plasma ACTH levels. This is achieved by inhibiting the firing of dorsal raphe 5-HT neurones. WAY 100635 produces anxiolytic-like effects in the mouse light/dark box anxiety model. In the delayed-matching-to-position model of rat short-term memory, WAY 100635 reverses the disruptive effects of 8-OH-DPAT on motor motivational performance but has no intrinsic effect on cognition.[2] In the anesthetized rat, WAY 100635 inhibits the inhibitory action of 8-OH-DPAT on dorsal raphe neuronal firing at doses that have no inherent inhibitory effect. In behavioral models, WAY 100635 does not directly cause any overt behavioral changes in rats or guinea pigs, but it effectively counteracts the behavioral syndrome caused by 8-OH-DPAT (minimum effective dose = 0.003 mg/kg s.c. and ID50 = 0.01 mg/kg s.c., respectively). With ID50 values of 0.01 mg/kg s.c., WAY 100635 also prevents the hypothermia that is brought on by 8-OH-DPAT in rats and mice.[4]
Cell Assay
Extracellular recordings are performed using glass microelectrodes that have been loaded with 2 M NaC1 (12 MΩ–15 MΩ). Two or three-millisecond biphasic action potentials, slow (0.5 Hz - 2.0 Hz) discharge patterns, and regular discharge patterns are characteristics that distinguish cells as 5-HT neurons. The alpha-l adrenergic agonist phenylephrine (3 μM) is added to the superfusing ACSF to cause firing in the otherwise silent neurons. Prior to applying the various medications, baseline activity is tracked for at least ten minutes. Precise action potentials coupled to an A/D converter and a PC drive individual action potentials that drive an oscilloscope, an electronic ratemeter, and a high-input impedance amplifier. The integrated firing rate is measured, calculated, and shown on a chart recorder as successive 10-sec samples using specialized software. Agonists' effects are assessed by comparing the mean discharge frequency recorded during the two minutes prior to WAY 100635 application with the frequency recorded at the peak of the drug's action, which is typically two to five minutes after application starts. The effect of the agonist is contrasted with the baseline firing rate and frequency observed during the antagonist's single superfusion when the agonists are applied in the presence of the antagonist. Before retesting the agonists' action, the antagonist is given ten to twenty-five minutes to acclimate.
Animal Protocol
Dissolved in 0.9% NaCl; 250 μL (30.4 μCi/mL); i.v. injection
Male CD1 mice with 25-30 g body weight
References

[1]. J Pharmacol Exp Ther . 1996 Aug;278(2):679-88.

[2]. Behav Brain Res . 1996;73(1-2):337-53.

[3]. Brain Res . 1997 Jan 16;745(1-2):96-108.

[4]. Eur J Pharmacol . 1995 Jul 25;281(1):81-8.

[5]. Eur J Pharmacol . 1994 Dec 27;271(2-3):505-14.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H38N4O6
Molecular Weight
538.64
Exact Mass
538.28
Elemental Analysis
C, 64.67; H, 7.11; N, 10.40; O, 17.82
CAS #
1092679-51-0
Appearance
Solid powder
SMILES
COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.C(=C\C(=O)O)\C(=O)O
InChi Key
XIGAHNVCEFUYOV-BTJKTKAUSA-N
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-
Chemical Name
(Z)-but-2-enedioic acid;N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide
Synonyms
WAY 100635 Maleate; WAY-100635; WAY100635
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~85 mg/mL (~157.8 mM)
Water: <1 mg/mL
Ethanol: ~85 mg/mL (~157.8 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.8565 mL 9.2826 mL 18.5653 mL
5 mM 0.3713 mL 1.8565 mL 3.7131 mL
10 mM 0.1857 mL 0.9283 mL 1.8565 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Biological Data
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