(S)-WAY 100135 dihydrochloride
目录号 : GC14805A 5-HT1A receptor antagonist
Cas No.:149007-54-5
Sample solution is provided at 25 µL, 10mM.
(S)-WAY 100135 dihydrochloride is a potent and selective antagonist of 5-HT1A receptor with IC50 value of 15 nM.
The 5-HT1A receptor is a G protein-coupled receptor for endogenous neurotransmitter serotonin (5-HT) and mediates inhibitory neurotransmission.
(S)-WAY 100135 dihydrochloride is a potent and selective somatodendritic and postsynaptic 5-HT1A receptors antagonist. (+/-)-WAY100135 inhibited 5-HT1A receptor in the rat hippocampal with IC50 value of 34 nM [1].
In the murine elevated plus-maze test, (S)-WAY 100135 (10 mg/kg) exhibited anxiolytic-like effects [2]. In free feeding rats, WAY-100135 (3 mg/kg) significantly inhibited hyperphagia and the increased incidence of feeding induced by 8-OH-DPAT (0.1 mg/kg), which was mediated by somatodendritic 5-HT1A autoreceptor [3]. In rats, (S)-WAY 100135 (0.2, 1, 5 ug/ul) inhibited the impairment of choice accuracy induced by intrahippocampal scopolamine (3.75 ug/ul) in a dose-dependent way. However, (S)-WAY 100135 didn’t influence the acquisition of spatial learning [4]. In rats, WAY-100135 (10.0 mg/kg) inhibited the decrease of 5-HT release induced by buspirone, a 5-HT1A receptor partial agonist [5].
References:
[1]. Fletcher A, Bill DJ, Bill SJ, et al. WAY100135: a novel, selective antagonist at presynaptic and postsynaptic 5-HT1A receptors. Eur J Pharmacol, 1993, 237(2-3): 283-291.
[2]. Rodgers RJ, Cole JC. Anxiolytic-like effect of (S)-WAY 100135, a 5-HT1A receptor antagonist, in the murine elevated plus-maze test. Eur J Pharmacol, 1994, 261(3): 321-325.
[3]. Hartley JE, Fletcher A. The effects of WAY-100135 and 8-hydroxy-2-(di-n-propylamino)tetralin on feeding in the rat. Eur J Pharmacol, 1994, 252(3): 329-332.
[4]. Carli M, Luschi R, Samanin R. (S)-WAY 100135, a 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine. Eur J Pharmacol, 1995, 283(1-3): 133-139.
[5]. Routledge C, Gurling J, Ashworth-Preece MA, et al. Differential effects of WAY-100135 on the decrease in 5-hydroxytryptamine release induced by buspirone and NAN-190. Eur J Pharmacol, 1995, 276(3): 281-284.
Cas No. | 149007-54-5 | SDF | |
化学名 | (S,Z)-N-(tert-butyl)-3-(4-(2-methoxyphenyl)piperazin-1-yl)-2-phenylpropanimidic acid dihydrochloride | ||
Canonical SMILES | CC(C)(/N=C(O)/[C@](C1=CC=CC=C1)([H])CN2CCN(C3=CC=CC=C3OC)CC2)C.Cl.Cl | ||
分子式 | C24H33N3O2.2HCl | 分子量 | 468.47 |
溶解度 | <46.85mg/ml 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。 |
||
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1346 mL | 10.673 mL | 21.3461 mL |
5 mM | 0.4269 mL | 2.1346 mL | 4.2692 mL |
10 mM | 0.2135 mL | 1.0673 mL | 2.1346 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet