1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. (±)-Epibatidine

(±)-Epibatidine  (Synonyms: CMI 545)

目录号: HY-101078
产品使用指南 技术支持

(±)-Epibatidine 是一种烟碱激动剂。(±)-Epibatidine 是神经元 nAChR 激动剂。

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(±)-Epibatidine Chemical Structure

(±)-Epibatidine Chemical Structure

CAS No. : 148152-66-3

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规格 是否有货
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100 mg   询价  
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Customer Review

Other Forms of (±)-Epibatidine:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

(±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist.

IC50 & Target

nAChR[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.01 μM
Compound: 2
Agonist activity at recombinant human alpha-3-beta-4 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
Agonist activity at recombinant human alpha-3-beta-4 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
[PMID: 17929796]
HEK293 EC50
0.05 μM
Compound: 2
Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
Agonist activity at recombinant human alpha-4-beta-2 nAChR expressed in HEK293 cells assessed as induction of calcium influx by FLIPR assay
[PMID: 17929796]
IMR-32 EC50
0.027 μM
Compound: epibatidine
Agonist activity at human recombinant alpha3beta4 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay
Agonist activity at human recombinant alpha3beta4 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay
[PMID: 19232492]
IMR-32 IC50
0.076 nM
Compound: epibatine
Displacement of [I125]Epibatidine from nAChR in human IMR32 cells after 60 mins
Displacement of [I125]Epibatidine from nAChR in human IMR32 cells after 60 mins
[PMID: 23403082]
IMR-32 EC50
0.12 μM
Compound: epibatidine
Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay
Agonist activity at human recombinant alpha4beta2 nAChR expressed in human IMR32 cells assessed as calcium dynamics by FLIPR assay
[PMID: 19232492]
体外研究
(In Vitro)

Intracerebroventricular injection of (±)-Epibatidine (0.1 μg) significantly increases intercontraction interval (ICI) but does not change pressure threshold (PT) or maximal voiding pressure (MVP), whereas 1 μg of (±)-Epibatidine increases PT and MVP (P<0.05) and decreased ICI. A low intravenous dose of (±)-Epibatidine (0.001-0.1 μg) has no effect; however, a large dose of (±)-Epibatidine (1 μg) significantly decreases ICI and increases MVP (P<0.05) but does not change PT (P>0.05). (±)-Epibatidine has not only a potent stimulatory effect on nAChR subtypes in the brain (α4β2) but also in sympathetic and parasympathetic ganglia (α3β4) and at the neuromuscular junction (α1β1γδ) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

208.69

Formula

C11H13ClN2

CAS 号
中文名称

(±)-地棘蛙素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(±)-Epibatidine
目录号:
HY-101078
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