Description: Potent, 5-HT1A silent antagonist. Also D4 agonist
Chemical Name:N-[2-[4-(2-Methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexanecarboxamide maleate
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent, silent antagonist of 5-HT1A receptors (IC50 = 2.2 nM; Ki = 0.84 nM for rat 5-HT1A receptors). Displays 100-fold selectivity for 5-HT1A over other 5-HT subtypes. Also exhibits agonist activity at dopamine D4 receptors.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
water
13.47
25
Preparing Stock Solutions
The following data is based on the product molecular weight 538.64. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.86 mL
9.28 mL
18.57 mL
5 mM
0.37 mL
1.86 mL
3.71 mL
10 mM
0.19 mL
0.93 mL
1.86 mL
50 mM
0.04 mL
0.19 mL
0.37 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Mensonides-Harsemaet al (2000) Synthesis and in vitro and in vivo functional studies of ortho-substituted phenylpiperazine and N-substituted 4-N-(o-methoxyphenyl)aminopiperidine analogues of WAY100635. J.Med.Chem. 43 432 PMID: 10669570
Zhuanget al (1994) Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2''-pyridinyl)-p-iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand. J.Med.Chem. 37 1406 PMID: 8182697
Forsteret al (1995) A pharmacological profile of the selective silent 5-HT1A receptor antagonist, WAY-100635. Eur.J.Pharmacol. 281 81 PMID: 8566121
Chemelet al (2006) WAY-100635 is a potent dopamine D4 receptor agonist. Psychopharmacology (Berl). 188 244 PMID: 16915381