WAY100635 Chemical Properties

storage temp. 

Store at -20°C

solubility 

≥53.9 mg/mL in DMSO; ≥51.2 mg/mL in EtOH; ≥6.08 mg/mL in H2O with ultrasonic

form 

solid

color 

White to off-white

Water Solubility 

Soluble to 25 mM in water

Safety Information

HS Code 

2933.59.8000

WAY100635 Usage And Synthesis

Description

WAY-100635 is a potent, silent antagonist of serotonin 5-HT_1A receptors with an IC₅₀ value of 2.2 nM (K_i = 0.8 nM) for inhibiting 5-HT_1A receptors in rat hippocampal membranes. Because it displays 100-fold selectivity for 5-HT_1A over other 5-HT subtypes, WAY-100635 is classically used to examine the distribution and function of 5-HT_1A receptors. However, WAY-100635 has also been shown to exhibit agonist activity at dopamine D₄ receptors (K_d = 2.4 nM).

Uses

WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist[1][2][3].

in vivo

IC 50

D₄ Receptor; sPLA2: 8.87 (pIC₅₀); sPLA2: 9.71 (pA2)

storage

Desiccate at RT

References

[1] Chemel BR, et al. WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51. DOI:10.1007/s00213-006-0490-4
[2] Mannucci C, et al. Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats. Phytomedicine. 2012 Sep 15;19(12):1117-24. DOI:10.1016/j.phymed.2012.07.001
[3] Al Hussainy R, et al. Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinatedanalogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor. J Med Chem. 2011 May 26;54(10):3480-91. DOI:10.1021/jm1009956

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