CAS 162760-96-5|WAY-100635

Introduction:Basic information about CAS 162760-96-5|WAY-100635, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameWAY-100635
CAS Number162760-96-5Molecular Weight422.56300
Density/Boiling Point/
Molecular FormulaC25H34N4O2Melting Point/
MSDS/Flash Point/

Names

NameN-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide
SynonymMore Synonyms

WAY-100635 BiologicalActivity

DescriptionWAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
Related CatalogSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT ReceptorResearch Areas >>Neurological Disease
Target

5-HT1A Receptor:8.87 (pIC50)

5-HT1A Receptor:9.71 (pA2)

In VitroWAY-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. WAY-100635 displaces specific binding of the 5-HT1A radioligand, [3H]8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tetralin), to rat hippocampal membranes with a plCIC50 of 8.87[1].
In VivoAdministration of (S)-WAY-100135 (0.025-1.0 mg/kg i.v.) moderately depresses neuronal activity at all doses tested. In contrast, administration of WAY-100635 (0.025-0.5 mg/kg i.v.) significantly increases neuronal activity. The stimulatory action of WAY-100635, like that of spiperone, is evident during wakefulness but not during sleep. Pretreatment with (S)-WAY-100135 (0.5 mg/kg i.v.) weakly attenuates the inhibitory action of 8-hydroxy-2-(di-n-propylamino) tetralin. In contrast, WAY-100635 at doses as low as 0.1 mg/kg i.v. completely blockes the action of 8-hydroxy-2-(di-n-propylamino) tetralin. The antagonist action of WAY-100635 at 5-HT1A autoreceptors closely parallels its ability to increase neuronal activity. Overall, WAY-100635 appears to act as a selective 5-HT1A antagonist, whereas (S)-WAY-100135 does not. The results obtained with WAY-100635 confirm our previous findings obtained with spiperone and further support the hypothesis that 5-HT1A autoreceptor-mediated feedback inhibition operates under physiological conditions[2].
References

[1]. Forster EA, et al. A pharmacological profile of the selective silent 5-HT1A receptor antagonist, WAY-100635. Eur J Pharmacol. 1995 Jul 25;281(1):81-8.

[2]. Fornal CA, et al. WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135. J Pharmacol Exp Ther. 1996 Aug;278(2):752-62.

Chemical & Physical Properties

Molecular FormulaC25H34N4O2
Molecular Weight422.56300
Exact Mass422.26800
PSA48.91000
LogP3.82860
InChIKeySBPRIAGPYFYCRT-UHFFFAOYSA-N
SMILESCOc1ccccc1N1CCN(CCN(C(=O)C2CCCCC2)c2ccccn2)CC1
Storage condition-20°C

Synonyms

Lopac-W-108
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)-cyclo-hexanecarboxamide
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexanecarboxamide maleate
cyclohexanecarboxamide,n-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-n-2-pyridinyl
N-{2-[4-(methoxyphenyl)-1-piperazinyl]ethyl}-N-(2-pyridinyl)-cyclohexanecarboxamide
WAY-100635
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