WAY-100635

Modify Date: 2024-01-02 19:38:45

WAY-100635 Structure
WAY-100635 structure
Common Name WAY-100635
CAS Number 162760-96-5 Molecular Weight 422.56300
Density N/A Boiling Point N/A
Molecular Formula C25H34N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of WAY-100635


WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.

 Names

Name N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide
Synonym More Synonyms

 WAY-100635 Biological Activity

Description WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
Related Catalog
Target

5-HT1A Receptor:8.87 (pIC50)

5-HT1A Receptor:9.71 (pA2)

In Vitro 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. 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 Vivo Administration 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 Formula C25H34N4O2
Molecular Weight 422.56300
Exact Mass 422.26800
PSA 48.91000
LogP 3.82860
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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