Alniditan (Alnitidan)
(Synonyms: Alnitidan) 目录号 : GC31054
Alniditan (Alnitidan) (Alnitidan) 是一种有效的 5-HT1B 和 5-HT1D 受体激动剂，在 HEK293 细胞中对 h5-HT1B 和 h5-HT1D 受体的 IC50 分别为 1.7 nM 和 1.3 nM。
Cas No.:152317-89-0
Sample solution is provided at 25 µL, 10mM.
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Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
In vitro, alniditan exhibits little vasoconstrictive effects on the rat basilar artery, although at a very high concentration 1 mM, alniditan causes intensive constriction, most likely through a mechanism independent from 5-HT receptor activation[1]. Alniditan is 10 times more potent than sumatriptan at the h5-HT1B receptor, and twice as potent at the h5-HT1D receptor[3].
The intraperitoneal administration of alniditan ED50=9 μg/kg and sumatriptan ED50=70 μg kg dose dependly reduces [125I]-BSA extravasation in the rat meninges when done 30 min before stimulation. The estimated ED values for alniditan are 9 μg/kg in the absence and 190 μg/kg in the presence of GR 127935[1]. Alniditan (3, 10, 30 and 100 μg/kg) produces a dose-dependent increase in the arteriovenous oxygen saturation difference, which seems to be attenuated in animals treated with GR127935. Alniditan dose-dependently decreases total carotid and arteriovenous anastomotic blood flow and concomitant conductance values; nutrient blood flow and conductance increase. Alniditan also produces significant increases in vascular conductance to the skin, ear, bone, salivary gland, fat, tongue, brain and dura mater; no changes are observed in the muscles and eyes[2].
[1]. Limmroth V, et al. Effects of alniditan on neurogenic oedema in the rat dura mater and on contraction of rat basilar artery. Eur J Pharmacol. 1999 Oct 8;382(2):103-9. [2]. De Vries P, et al. The antimigraine agent alniditan selectively constricts porcine carotid arteriovenous anastomoses via 5-HT1B/1D receptors. Eur J Pharmacol. 1998 Jun 19;351(2):193-201. [3]. Lesage AS, et al. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol. 1998 Apr;123(8):1655-65.
Animal experiment: | After a stabilisation period of about 1 h, the animals are divided into three groups. In the first group (n=4), values of heart rate, mean arterial blood pressure, carotid blood flow and its distribution, as well as arterial and jugular venous blood gases are measured at baseline, and after four consecutive injections of physiological saline (0.5 mL, every 20 min). The second and third groups of animals (n=6 each) are pre-treated with saline (i.v.) or GR127935 (0.5 mg/kg, i.v.), respectively, given over a period of 5 min at a rate of 1 mL/min. After a waiting period of 15 min, baseline values of heart rate, mean arterial blood pressure, carotid blood flow and its distribution, as well as arterial and jugular venous blood gases are measured. Subsequently, these groups of animals receive sequential i.v. doses of alniditan (3, 10, 30 and 100 μg/kg) every 20 min. Fifteen minutes after each dose of alniditan, all haemodynamic variables are assessed again. |
References: [1]. Limmroth V, et al. Effects of alniditan on neurogenic oedema in the rat dura mater and on contraction of rat basilar artery. Eur J Pharmacol. 1999 Oct 8;382(2):103-9. | |
| Cas No. | 152317-89-0 | SDF | |
| 别名 | Alnitidan | ||
| Canonical SMILES | C1(NCCCNC[C@H]2CCC3=CC=CC=C3O2)=NCCCN1 | ||
| 分子式 | C17H26N4O | 分子量 | 302.41 |
| 溶解度 | Soluble in DMSO | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3068 mL | 16.5338 mL | 33.0677 mL |
| 5 mM | 0.6614 mL | 3.3068 mL | 6.6135 mL |
| 10 mM | 0.3307 mL | 1.6534 mL | 3.3068 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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