WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i 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].

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D_2L or D_4.4 receptors^[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D_2L, D₃, and D_4.2 receptors, respectively. Saturation analyses demonstrat that the K_d of [³H] WAY-100635 at D_4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D_4.4 cells with EC₅₀ of 9.7 nM. WAY-100635 possesses high affinity for D_4.4 receptor (3.3 nM) ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Chemel BR, et al. WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 2006 Oct;188(2):244-51.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]