WAY-100635 Maleate是一种有效的，选择性的5-HT1A受体拮抗剂，其 IC50 值为 0.91 nM，Ki 值为 0.39 nM，pIC50为8.87，比作用于其他5-HT受体亚型和主要的神经递质受体选择性高100倍以上。此外，WAY-100635 maleate 也是一种有效的多巴胺 D4 受体激动剂。
WAY-100635 is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 ?0.12 nM for 5-HT. Intravenous administration of WAY-100635 (0.025-0.5 mg/kg) markedly improved neuronal activity. The stimulatory action of WAY-100635 was evident during wakefulness (when serotonergic neurons typically display a relatively high level of activity) but not during sleep (when serotonergic neurons display little or no spontaneous activity). WAY-100635 at doses as low as 0.1 mg/kg i.v. completely blocked the action of 8-hydroxy-2- (di-n-propylamino)tetralin. The antagonist action of WAY-100635 at 5-HT1A autoreceptors closely paralleled its ability to increase neuronal activity. WAY-100635 affected neither the blackage of action potential frequency adaptation and slow afterhyperpolarization produced by 5-HT (15 μM) nor the hyperpolarization and decrease in membrane input resistance evoked by bath application of GABA (B) receptor agonist baclofen (10 μM).
| 体外实验* | |
|---|---|
| 细胞系 | Neurons |
| 方法 | Making extracellular recordings with glass microelectrodes filled with 2 M NaC1 (12 MΩ-15 MΩ). Identifing the cells as 5-HT neurons according to the following criteria: biphasic action potentials of 2 msec to 3 msec in duration, slow (0.5 Hz - 2.0 Hz) and regular pattern of discharge. Firing is evoked in the otherwise silent neurons by adding the alpha-l adrenergic agonist phenylephrine (3 μM) to the superfusing ACSF. Recoring baseline activity for at least 10 minutes before application of the different drugs. The electric signals are fed into a high-input impedance amplifier, an oscilloscope and an electronic ratemeter triggered by individual action potentials connected to an A/D converter and a personal computer. Using dedicated software, the integrated firing rate is recorded, computed and displayed on a chart recorder as consecutive 10-sec samples. Evaluting the effects of agonists by comparing the mean discharge frequency recorded during the 2 minutes that preceded WAY 100635 application with that recorded at the peak of WAY 100635 action (usually 2-5 minutes after the beginning of application). When the agonists are applied in the presence of the antagonist, the effect of the agonist is compared to baseline firing rate and to the frequency recorded during superfusion of the antagonist alone. The antagonist is left to equilibrate for 10 minutes to 25 minutes before retesting of the action of agonists. |
| 浓度 | 1 nM -5 nM |
| 处理时间 | 2 minutes -5 minutes |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 体内实验* | |
|---|---|
| 动物模型 | Male CD1 mice with 25-30 g body weight |
| 配制 | 0.9% NaCl |
| 剂量 | 250 μL (30.4 μCi/mL) |
| 给药处理 | Administered via i.v. |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 分子量 | 538.64 |
| 分子式 | C25H34N4O2.C4H4O4 |
| CAS号 | 1092679-51-0 |
| 溶解性（25°C） | DMSO ≥ 100 mg/mL Water 20 mg/mL |
| 储存条件 | -20°C, dry, sealed |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.8565 mL | 9.2826 mL | 18.5653 mL |
| 5 mM | 0.3713 mL | 1.8565 mL | 3.7131 mL |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8565 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
| 其他相关的5-HT Receptor产品 |
|---|
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TC-2153 是一种纹状体富集蛋白酪氨酸磷酸酶 (STEP) 的选择性抑制剂。TC-2153 也抑制 5-HT2A 受体介导的信号传递。 |
| Gentisein
Gentisein (NSC-329491) 是 Mangiferin 的主要代谢物，有效抑制 5-HT 的摄取，IC50为 4.7 µM。 |
| MM120
MM120 是一种合成色胺，同时也是5-羟色胺2A（5-HT2A）受体的部分激动剂。可用于GAD和注意缺陷多动障碍（ADHD）的相关研究。 |
| SB 258741 hydrochloride
SB 258741 hydrochloride是一种特异性的 5-HT7 受体拮抗剂，可用于精神分裂症的研究。 |
| 5-HT1A antagonist 1
5-HT1A antagonist 1是一种有效和选择性的 5-HT1A受体拮抗剂，Ki 值为 35 nM。5-HT1A antagonist 1 可用于中枢神经系统疾病的研究。 |
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