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

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

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(±)-Epibatidine Chemical Structure

(±)-Epibatidine Chemical Structure

CAS No. : 148152-66-3

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Other Forms of (±)-Epibatidine:

(±)-Epibatidine Related Antibodies

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Description

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

IC50 & Target

nAChR[1]
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]
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].

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

(±)-Epibatidine Related Antibodies
Molecular Weight

208.69

Formula

C11H13ClN2
CAS No.
SMILES

ClC1=CC=C([C@H]2[C@@H](N3)CC[C@@H]3C2)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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.
References
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(±)-Epibatidine Related Classifications

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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.

Keywords:

(±)-Epibatidine148152-66-3CMI 545CMI545CMI-545nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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