5-HT₃ Receptor

体外活性：昂丹司琼可降低戒断症状的强度，如排便增多、跳跃和湿狗颤抖，提高伤害感受阈值（因突然戒断而降低），但不会改变排尿、直肠温度或唾液分泌。昂丹司琼和格拉司琼显着增强玻璃珠的胃排空，并改善顺铂引起的大鼠胃排空减慢。 Ondansetron 在小鼠中表现出双相剂量反应特征，在强迫游泳和悬尾测试中，抗抑郁样作用在 0.1 mg/kg 时达到峰值。昂丹司琼预处理可增强氟西汀和文拉法辛的抗抑郁作用，但不影响地昔帕明或 8-羟基-2-(二正丙氨基)四氢化萘的作用。 Ondansetron (10 mg/kg) 可逆转开放区域的多动症，并减少进入高架十字迷宫的开放臂的百分比和花费的时间。 Ondansetron 是一种选择性强效 5HT3 受体拮抗剂，在 0.01 mg/kg 剂量下可有效阻断安非他明诱导的 LI 破坏，但在 0.1 mg/kg 剂量下则无效。昂丹司琼能够减弱多巴胺活性的增加，与安非他明产生药理作用，而不影响基线多巴胺活性。昂丹司琼可促进年轻成年和老年动物的表现，并抑制由东莨菪碱、电损伤或大细胞基底核的鹅膏蕈酸损伤引起的习惯损害。昂丹司琼和槟榔碱可对抗东莨菪碱引起的损伤。细胞测定：5-HT 诱发瞬时内向电流（EC50 = 3.4 microM；希尔系数 = 1.8），该电流被 5-HT3 受体拮抗剂昂丹司琼 (ondansetron) 阻断 (IC50 = 103 pM)。 5-HT3A 受体拮抗剂昂丹司琼 (ondansetron) (0.3 nM) 可逆性抑制 5-HT (30 microM) 信号达 70%，3 nM 时可消除该反应。

测试的最低剂量（0.1 mg/kg，IP）的急性昂丹司琼给药没有效果，而其他剂量（0.33和1 mg/kg，IP）则对听觉门控产生改善。在一天中的固定时间腹腔内（ip）注射不同剂量的昂丹司琼，以确定亚致死（TD50）和致死（LD50）剂量，分别为3.7 +/- 0.6 mg/kg和4.6 +/- 0.5毫克/公斤。在注射攻击剂量的乙醇（2.4 g/kg，腹膜内）之前给予昂丹司琼（0.25-1.0 mg/kg，皮下），显着且剂量依赖性地减弱致敏的表达。此外，在第 1、4、7 和 10 天乙醇注射前给予昂丹司琼（1.0 mg/kg，皮下注射）可显着阻断致敏的发展（第 1、4、7 和 10 天）和表达（第 15 天）乙醇注射的运动兴奋作用。

Ondansetron 是 5-HT3 受体拮抗剂，可抑制 5-HT 引起的瞬时内向电流（EC50 = 3.4 microM；Hill 系数 = 1.8）（IC50 = 103 pM）。 Ondansetron 是一种 5-HT3A 受体拮抗剂，在 0.3 nM 时可逆性抑制 5-HT (30 microM) 信号 70%，在 3 nM 时完全消除反应。

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Ondansetron is frequently used for nausea during and after cesarean section, usually in doses of 4 to 8 mg intravenously. Use during and after cesarean section appears to not affect the onset of breastfeeding. No adverse infant effects have been reported in this setting or among women who received ondansetron postpartum in a pharmacokinetic study. Use of ondansetron in nursing mothers beyond the immediate postpartum setting has not been studied well, but the drug is labeled for use in infants as young as 1 month of age. A computer model demonstrated that the amounts in milk are much less than this dose. No special precautions are required.
◉ Effects in Breastfed Infants
In a pharmacokinetic study of 78 women who received ondansetron intravenously postpartum, no adverse effects were reported in their breastfed infants.
◉ Effects on Lactation and Breastmilk
A randomized, double-blind study compared placebo to intravenous ondansetron 4 mg given after cesarean section as prophylaxis for postoperative nausea and vomiting. There was no difference in the time of the first breastfeeding between the two groups.
In a retrospective study of women undergoing cesarean section deliveries, 3 regimens were compared: dexmedetomidine before anesthesia and during delivery (n = 115), normal saline before anesthesia and during delivery and dexmedetomidine after delivery (n = 109), and normal saline before anesthesia and during delivery (n = 168). All women received ondansetron 4 mg as needed and before removal of sutures. The average total amount of ondansetron consumed in the women ranged from 6 mg to 9 mg in the various groups. The time to first production of milk was similar in all groups (25 to 28 minutes).

[1]. Ondansetron, dexamethasone and an NK1 antagonist block radiation sickness in mice. Pharmacol Biochem Behav. 2005 Sep;82(1):24-9.

[2]. Ondansetron. A review of its pharmacology and preliminary clinical findings in novel applications. Drugs. 1996 Nov;52(5):773-94.

Ondansetron Hydrochloride is the hydrochloride salt of the racemic form of ondansetron, a carbazole derivative and a selective, competitive serotonin 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist with antiemetic activity. Although its mechanism of action has not been fully characterized, ondansetron appears to competitively block the action of serotonin at 5HT3 receptors peripherally in the gastrointestinal tract as well as centrally in the area postrema of the CNS, where the chemoreceptor trigger zone (CTZ) for vomiting is located, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.
See also: Ondansetron (has active moiety).

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Drug Indication
Treatment of alcohol use disorder

C18H19N3O

329.82

329.129

C, 65.55; H, 6.11; Cl, 10.75; N, 12.74; O, 4.85

99614-01-4

Ondansetron hydrochloride dihydrate; 103639-04-9; Ondansetron; 99614-02-5; Ondansetron-d3 hydrochloride; 1346605-02-4; Ondansetron-d6 hydrochloride; 1225442-22-7

68647

Solid powder

1.27g/cm3

546ºC at 760mmHg

178.5-179.5ºC

284ºC

3.93

39.82

1

2

2

23

440

0

O=C1C(CN2C=CN=C2C)CCC(N3C)=C1C4=C3C=CC=C4.[H]Cl

MKBLHFILKIKSQM-UHFFFAOYSA-N

InChI=1S/C18H19N3O.ClH/c1-12-19-9-10-21(12)11-13-7-8-16-17(18(13)22)14-5-3-4-6-15(14)20(16)2;/h3-6,9-10,13H,7-8,11H2,1-2H3;1H

9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-carbazol-4-one;hydrochloride

GR 38032F; GRC 50775; SN 307; GR-38032F; GRC-50775; SN-307; GR38032F; GRC50775; SN307; GR 38032F; trade name: Zofran

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
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7、 以上所有助溶剂都可在 Invivochem.cn网站购买。