(±)-Epibatidine
(Synonyms: CMI 545) 目录号 : GC14410
An agonist of α4β2 subunit-containing nAChRs
Cas No.:148152-66-3
Sample solution is provided at 25 µL, 10mM.
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(+)-AJ 76 hydrochloride is an antagonist of dopamine autoreceptor with pKi values of 6.95, 6.67, 6.37, 6.21 and 6.07 for hD3, hD4, hD2S, hD2L and rD2 receptors, respectively.
Dopamine receptor is a G protein-coupled receptor and mainly exists in the vertebrate central nervous system (CNS). Dopamine receptor is a receptor for dopamine and plays a critical role in memory, learning, pleasure, cognition, motivation and fine motor control.
(+)-AJ 76 hydrochloride is a dopamine receptor antagonist. In rats, AJ76 stimulated locomotor activity and increased the levels of 3,4-dihydroxyphenylacetic acid (DOPAC) and HVA in brain, which were dopamine metabolites [1]. In rats injected with cocaine, (+)-A J76 increased the locomotor stimulation during the first 30 min. However, (+)-AJ76 inhibited the later more intense locomotor stimulation and cocaine-induced stereotypies [2]. In vivo, (+)-AJ76 induced dopamine release mainly through interaction with dopamine receptors in the terminal regions of the A9 and A10 dopaminergic fibers. However, (+)-AJ76 increased the level of DOPAC via the somatodendritic autoreceptors [3].
References:
[1]. Kullingsjö H, Carlsson A, Svensson K. Effects of repeated administration of the preferential dopamine autoreceptor antagonist, (+)-AJ76, on locomotor activity and brain DA metabolism in the rat. Eur J Pharmacol, 1991, 205(3): 241-246.
[2]. Piercey MF, Lum JT, Hoffmann WE, et al. Antagonism of cocaine's pharmacological effects by the stimulant dopaminergic antagonists, (+)-AJ76 and (+)-UH232. Brain Res, 1992; 588(2): 217-222.
[3]. Waters N, Hansson L, Löfberg L, et al. Intracerebral infusion of (+)-AJ76 and (+)-UH232: effects on dopamine release and metabolism in vivo. Eur J Pharmacol, 1994, 251(2-3): 181-190.
Animal experiment: | Rats[1]Voiding is studied in urethane-anesthetized (1.2 g/kg sc) or awake female Sprague-Dawley rats (250-300 g). In all experiments, control cystometrograms (CMGs) are recorded for ~2 h before intracerebroventricular and intravenous injection of vehicle or (±)-Epibatidine solutions. Dose-response curves are constructed by administering increasing doses of (±)-Epibatidine [0.001-1 μg in 1 μL intracerebroventricularly (icv); 0.001-1 μg in 200 μL iv] at 30-min to 2-h intervals. (±)-Epibatidine is administered ~30 min after vehicle (aCSF, 1 μL icv; or saline solution, 200 μL iv). Chlorisondamine (10 μg, 1 μL icv) is injected 10-30 min before (±)-Epibatidine via the intracerebroventricular route in some experiments to block the effect of the agonist. The intravesical pressure to induce micturition (PT), MVP, and intercontraction interval (ICI; the interval between voids or reflex bladder contractions) are measured and converted into percent change from control values[1]. |
References: [1]. Lee SJ, et al. Effect of (+/-)-epibatidine, a nicotinic agonist, on the central pathways controlling voidingfunction in the rat. Am J Physiol Regul Integr Comp Physiol. 2003 Jul;285(1):R84-90. | |
| Cas No. | 148152-66-3 | SDF | |
| 别名 | CMI 545 | ||
| 化学名 | (1S,2S,4R)-2-(6-chloropyridin-3-yl)-7-azabicyclo[2.2.1]heptane | ||
| Canonical SMILES | ClC(N=C1)=CC=C1[C@H]2[C@H](CC3)N[C@H]3C2 | ||
| 分子式 | C11H13ClN2 | 分子量 | 208.69 |
| 溶解度 | <24.55mg/ml in ethanol | 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 | 4.7918 mL | 23.959 mL | 47.918 mL |
| 5 mM | 0.9584 mL | 4.7918 mL | 9.5836 mL |
| 10 mM | 0.4792 mL | 2.3959 mL | 4.7918 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