ホーム>>Signaling Pathways>> Neuroscience>> nAChR>>(±)-Epibatidine

(±)-Epibatidine (Synonyms: CMI 545)

カタログ番号GC14410

ニコチン性アゴニスト

Products are for research use only. Not for human use. We do not sell to patients.

(±)-Epibatidine 化学構造

Cas No.: 148152-66-3

サイズ 価格 在庫数 個数
1mg
$99.00
Ship Within 7 Days
5mg
$371.00
Ship Within 7 Days

Tel:(909) 407-4943 Email: sales@glpbio.com

顧客レビュー

カスタマーレビューに基づきます。

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

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.

Background

(+)-AJ 76 hydrochlorideは、ドーパミン自己受容体の拮抗剤であり、hD3、hD4、hD2S、hD2LおよびrD2受容体に対するpKi値がそれぞれ6.95、6.67、6.37、6.21および6.07です。

ドーパミン受容体はGタンパク質共役受容体であり、主に脊椎動物の中枢神経系(CNS)に存在します。ドーパミン受容体はドーパミンの受容体であり、記憶、学習、快楽、認知能力、動機付けおよび細かい運動制御に重要な役割を果たしています。

(+)-AJ 76 hydrochlorideはドーパミン受容体拮抗薬です。ラットでは、AJ76は運動活性を刺激し、脳内のドーパミン代謝物である3,4-ジヒドロキシフェニル酢酸(DOPAC)とHVAのレベルを増加させました[1]。コカイン注射されたラットでは、(+)-A J76は最初の30分間における運動刺激を増強しましたが、後期のより強い運動刺激やコカイン誘発性ステレオタイプを抑制しました[2]。in vivoでは、(+)-AJ76は主にA9およびA10ドパミン神経繊維の末端領域に存在するドパミン受容体と相互作用してドパミン放出を誘起します。ただし、(+)-AJ76はソマトデンドリチック自己受容体を介してDOPACレベルを増加させます[3]。

References:
[1].  Kullingsj? 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, L?fberg 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.

Chemical Properties

Cas No. 148152-66-3 SDF
同義語 CMI 545
Chemical Name (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
Formula C11H13ClN2 M.Wt 208.69
溶解度 <24.55mg/ml in ethanol Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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
  • モルアリティ計算機

  • 希釈計算機

質量
=
濃度
x
容積
x
MW*
 
 
 
**ストックソリューションを準備する際には、常にバイアルラベルおよび MSDS/CoA(オンラインで利用可能)で掲載された製品のロット固有分子量を使用してください。

計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

レビュー

Review for (±)-Epibatidine

Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for (±)-Epibatidine

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.