WAY-100635 maleate salt

• CAT Number: I004393
• CAS Number: 634908-75-1
• Molecular Formula: C29H38N4O6
• Molecular Weight: 538.64
• Purity: ≥95%
• Target: 5-HT Receptor
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: Store at -20°C
• IC50: 0.95 nM

WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ± 0.12 nM for 5-HT.IC50 Value: 0.95 nMTarget: 5-HT Receptorin vitro: WAY 100635 has an IC50 of 1.35 nM and is > 100-fold selective for the 5-HT1A site relative to a range of other CNS receptors. The Bmax of [3H]WAY 100635 specific binding is consistently 50-60% greater than that of the agonist radioligand, [3H]8-OH-DPAT. Mn2+, but not guanine nucleotides, inhibits [3H]WAY 100635-specific binding. WAY 100635 has no 5-HT1A receptor agonist actions, but dose-dependently blocks the effects of agonists at both the postsynaptic 5-HT1A receptor in the CA1 region of the hippocampus, and the somatodendritic 5-HT1A receptor locates on dorsal raphe 5-HT neurones. [3H]WAY 100635 has a Kd of approximately 2.5 nM. In the isolated guinea-pig ileum 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.in vivo: WAY 100635 blocks the inhibitory action of 8-OH-DPAT on dorsal raphe neuronal firing in the anaesthetised rat at doses which has no inhibitory action per se. In behavioural models, WAY 100635 itself induces no overt behavioural changes but potently antagonises the behavioural syndrome induced by 8-OH-DPAT in the rat and guinea-pig (minimum effective dose = 0.003 mg/kg s.c. and ID50 = 0.01 mg/kg s.c., respectively). WAY 100635 also blocks the hypothermia induced by 8-OH-DPAT in the mouse and rat with ID50 values of 0.01 mg/kg s.c.

Reference

[1]. Al Hussainy, Rana; Design, Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of Bridgehead Iodinated Analogues 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. Journal of Medicinal Chemistry (2011), 54(10), 3480-3491.
[2]. Choi JY, Kim CH, Jeon TJ, Kim BS, Yi CH, Woo KS, Seo YB, Han SJ, Kim KM, Yi DI, Lee M, Kim DG, Kim JY, Lee KC, Choi TH, An G, Ryu YH.Effective microPET imaging of brain 5-HT(1A) receptors in rats with [(18) F]MeFWAY by suppression of radioligand defluorination.Synapse. 2012 Aug 28.
[3]. Mannucci C, Navarra M, Calzavara E, Caputi AP, Calapai G.Serotonin involvement in Rhodiola rosea attenuation of nicotine withdrawal signs in rats.Phytomedicine. 2012 Aug 23.
[4]. Katsidoni V, Anagnostou I, Panagis G.Cannabidiol inhibits the reward-facilitating effect of morphine: involvement of 5-HT(1A) receptors in the dorsal raphe nucleus.Addict Biol. 2012 Aug 2.
[5]. Paquette MA, Martinez AA, Macheda T, Meshul CK, Johnson SW, Berger SP, Giuffrida A.Anti-dyskinetic mechanisms of amantadine and dextromethorphan in the 6-OHDA rat model of Parkinson/’s disease: role of NMDA vs. 5-HT1A receptors.Eur J Neurosci. 2012 Aug 3.