WAY-100635是一种具有高效性选择的5-hydroxytryptamine 1A（5-HT1A）受体拮抗剂，IC50值为0.91nM，Ki值为0.39nM。
Cas No.:162760-96-5
Sample solution is provided at 25 µL, 10mM.
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WAY-100635 is a highly potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91nM and a Ki value of 0.39nM[1,2]. The 5-HT1A receptor is widely distributed in the central nervous system (e.g., hippocampus, amygdala) and peripheral nervous tissues (e.g., enteric nerves and cardiovascular system), playing a crucial role in regulating emotional states and the secretion of various hormones[3]. WAY-100635 is also a potent full agonist of the dopamine D4 receptor and is commonly used in positron emission tomography (PET) imaging, neuroscience, and behavioral and cognitive studies[4].
In vitro, pretreatment of human neuroblastoma SH-SY5Y cells with WAY-100635 (10μM) for 1h significantly inhibited the increase in cell viability induced by co-treatment with the antidepressant fluoxetine (1μM) and Aβo (5μM) for 24h[5]. In rat hippocampal homogenates, incubation with WAY-100635 (0.2μM) together with the 5-HT1A receptor agonist (+)-5-Me-8-OH-DPAT for 20min completely blocked the inhibition of forskolin-stimulated cAMP production induced by (+)-5-Me-8-OH-DPAT[6].
In vivo, subcutaneous injection of WAY-100635 (0.1mg/kg) in Albino Swiss mice 15min before treatment completely blocked the hypothermic effect induced by the 5-HT1A receptor agonist 8-OH-DPAT (5mg/kg)[7]. Intraperitoneal injection of WAY-100635 (0.1, 0.2, 0.4mg/kg) in chronic constriction injury (CCI) model mice receiving chrysin treatment dose-dependently reversed the alleviating effects of chrysin on heat hyperalgesia and mechanical allodynia[8].
References:
[1] FORNAL C A, METZLER C W, GALLEGOS R A, et al. WAY-100635, a potent and selective 5-hydroxytryptamine1A antagonist, increases serotonergic neuronal activity in behaving cats: comparison with (S)-WAY-100135[J]. The Journal of pharmacology and experimental therapeutics, 1996, 278(2): 752-762.
[2] AL HUSSAINY R, VERBEEK J, VAN DER BORN D, et al. 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[J]. Journal of medicinal chemistry, 2011, 54(10): 3480-3491.
[3] SAVITZ J, LUCKI I, DREVETS W C. 5-HT1A receptor function in major depressive disorder[J]. Progress in neurobiology, 2009, 88(1): 17-31.
[4] CLIFFE I A. A retrospect on the discovery of WAY-100635 and the prospect for improved 5-HT1A receptor PET radioligands[J]. Nuclear medicine and biology, 2000, 27(5): 441-447.
[5] YAMAMOTO K, TSUJI M, OGUCHI T, et al. Comparison of Protective Effects of Antidepressants Mediated by Serotonin Receptor in Aβ-Oligomer-Induced Neurotoxicity[J]. Biomedicines, 2024, 12(6): 1158.
[6] TRILLAT A C, MALAGIÉ I, MATHÉ-ALLAINMAT M, et al. Effects of WAY 100635 and (-)-5-Me-8-OH-DPAT, a novel 5-HT1A receptor antagonist, on 8-OH-DPAT responses[J]. European journal of pharmacology, 1998, 347(1): 41-49.
[7] WESOLOWSKA A, BORYCZ J, PALUCHOWSKA M H, et al. Pharmacological analysis of the hypothermic effects of NAN-190 and its analogs, postsynaptic 5-HT1A receptor antagonists, in mice[J]. Polish journal of pharmacology, 2002, 54(4): 391-399.
[8] WU J, WANG Y, CUI W, et al. 5-HT1A receptor-mediated attenuation of heat hyperalgesia and mechanical allodynia by chrysin in mice with experimental mononeuropathy[J]. Regional Anesthesia & Pain Medicine, 2020, 45(8): 610-619.
WAY-100635是一种具有高效性选择的5-hydroxytryptamine 1A（5-HT1A）受体拮抗剂，IC50值为0.91nM，Ki值为0.39nM[1,2]。5-HT1A广泛分布于中枢神经系统（如海马体、杏仁核）和外周神经组织（肠道神经及心血管系统）中，对调节情绪状态及多种激素的分泌均至关重要[3]。WAY-100635也是多巴胺D4受体的强效完全激动剂，通常用于正电子发射断层（PET）成像、神经科学及行为与认知研究[4]。
在体外，WAY-100635（10μM）预处理人类神经母细胞瘤SH-SY5Y细胞1h，显著抑制了由抗抑郁药fluoxetine（1μM）联合Aβo（5μM）处理24h所引起的细胞活力增加[5]。WAY-100635（0.2μM）处理大鼠海马组织匀浆，与5-HT1A受体激动剂(+)-5-Me-8-OH-DPAT共孵育20min，完全阻断了(+)-5-Me-8-OH-DPAT诱导的Forskolin刺激的cAMP生成抑制[6]。
在体内，WAY-100635（0.1mg/kg）通过皮下注射处理Albino Swiss小鼠15min，完全阻断了5-HT1A受体激动剂8-OH-DPAT（5mg/kg）诱导的低体温效应[7]。WAY-100635（0.1, 0.2, 0.4mg/kg）通过腹腔注射处理接受Chrysin治疗的慢性压迫损伤（CCI）模型小鼠，剂量依赖性地逆转了Chrysin对热痛觉过敏和机械性异常性疼痛的缓解作用[8]。
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells (human neuroblastoma) |
Preparation Method | SH-SY5Y cells were pretreated with 10μM WAY-100635 for 1h and incubated with 1μM fluoxetine and 5μM Aβo for 24h, then cell viability was assessed using the 3-(4, 5-dimethylthiazoyl-2-yl)-2-5, diphenyltetrazolium bromide (MTT) assay using the MTT Cell Count Kit. |
Reaction Conditions | 10μM; 1h |
Applications | WAY-100635 pretreatment significantly inhibited the increase in cell viability induced by the antidepressant fluoxetine combined with Aβo treatment. |
| Animal experiment [2]: | |
Animal models | Chronic constriction injury (CCI) C57BL/6J mice |
Preparation Method | CCI model mice that received oral Chrysin (30mg/kg; twice a day) for 2 weeks were given a single intraperitoneal injection of WAY-100635 (0.1, 0.2, 0.4 mg/kg) 30min before the scheduled Chrysin administration on the day of behavioral testing, followed by oral Chrysin administration as scheduled 30min later, and then behavioral assessments were performed. |
Dosage form | 0.1, 0.2, 0.4mg/kg; i.p. |
Applications | WAY-100635 treatment dose-dependently reversed the relieving effect of Chrysin on thermal hyperalgesia and mechanical dysphagia. |
References: | |
| Cas No. | 162760-96-5 | SDF | |
| 别名 | WAY 100635; WAY100635 | ||
| 化学名 | N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-pyridin-2-ylcyclohexanecarboxamide | ||
| Canonical SMILES | COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4 | ||
| 分子式 | C25H34N4O2 | 分子量 | 422.56 |
| 溶解度 | ≥ 42.3 mg/mL in DMSO, ≥ 134.2 mg/mL in EtOH | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3665 mL | 11.8326 mL | 23.6653 mL |
| 5 mM | 473.3 μL | 2.3665 mL | 4.7331 mL |
| 10 mM | 236.7 μL | 1.1833 mL | 2.3665 mL |
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