| Identification | Back Directory | [Name]
WAY100635 | [CAS]
1092679-51-0 | [Synonyms]
CS-998
WAY100635 100MG
WAY100635 USP/EP/BP
Cyclohexanecarboxamide, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-, (2Z)-2-butenedioate (1:1)
WAY-100635 (maleate) N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-cyclohexanecarboxamide, 2Z-butenedioate | [Molecular Formula]
C25H34N4O2.C4H4O4 | [MOL File]
1092679-51-0.mol | [Molecular Weight]
538.635 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Description]
WAY-100635 is a potent, silent antagonist of serotonin 5-HT1A receptors with an IC50 value of 2.2 nM (Ki = 0.8 nM) for inhibiting 5-HT1A receptors in rat hippocampal membranes. Because it displays 100-fold selectivity for 5-HT1A over other 5-HT subtypes, WAY-100635 is classically used to examine the distribution and function of 5-HT1A receptors. However, WAY-100635 has also been shown to exhibit agonist activity at dopamine D4 receptors (Kd = 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]
WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat[2]. | Animal Model: | Male Sprague-Dawley rats (220-240 g)[2] | | Dosage: | 1 mg/kg | | Administration: | Subcutaneous injection (Pharmacokinetic study) | | Result: | Reduced total abstinence score, increased immobility time and the burying behavior was increased.
|
| [IC 50]
D4 Receptor; sPLA2: 8.87 (pIC50); sPLA2: 9.71 (pA2) | [storage]
Store at -20°C | [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 |
|
|