(±)-Epibatidine
(±)-Epibatidine is a nicotinic agonist. (±)-Epibatidine is a neuronal nAChR agonist.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 148152-66-3
- 分子式: C11H13ClN2
- 分子量:208.69
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
nAChR[1]
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Cell Line
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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 | 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] |
| IMR-32 | EC50 |
0.7 μM
Compound: 1a(+)
|
Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor expressed in IMR32 cell
Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor expressed in IMR32 cell
|
[PMID: 16078832] |
| 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] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 148152-66-3
-
分子量 208.69
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分子式 C11H13ClN2
-
SMILES
ClC1=CC=C([C@H]2[C@@H](N3)CC[C@@H]3C2)C=N1
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別名
CMI 545
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)