2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Epiboxidine

Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Epiboxidine hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

Epiboxidine Chemical Structure

Epiboxidine Chemical Structure

CAS No. : 188895-96-7

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Other Forms of Epiboxidine:

Epiboxidine Related Antibodies

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Description

Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418[1].

IC50 & Target

Ki: 0.46 nM (rat α4β2 nAChR) and 1.2 nM (human α4β2 nAChR)[1]
In Vitro

Epiboxidine has affinity and functional at central neuronal α4β2 receptors, with Kis of 0.46 and 1.2 in rat and humen[1].
Epiboxidine has activity at ganglionic-type α3β4*-nicotinic receptors of PC12 cells, with a Ki of 19[1].
Epiboxidine is much less toxic than Epibatidine[1].
Epiboxidine stimulates sodium-22 influx in PC12 and TE671 cells, with EC50s of 0.18 and 2.6 µM[2].

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

Epiboxidine Related Antibodies
In Vivo

Epiboxidine (20 μg/kg; ip; once) treatment shows marked analgetic activity in mice[1].
Epiboxidine (50 and 100 mg/kg; intraperitoneal injected; once) causes marked antinociception as measured in the hot-plate assay[2].
Epiboxidine inhibits [3H]nicotine binding in rat cerebral cortical membranes, with a Ki of 0.6 nM[2].

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

Animal Model: Adult male NIH Swiss strain mice (25-30 g)[2]
Dosage: 50 and 100 mg/kg
Administration: I.p.; once
Result: Caused a dose-related Straub tail, hypomotility, hypoventilation and piloerection.
Molecular Weight

178.23

Formula

C10H14N2O
CAS No.
SMILES

CC1=NOC([C@@H]2[C@@H]3N[C@@H](CC3)C2)=C1
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
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Epiboxidine 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:

Epiboxidine188895-96-7nAChRNicotinic acetylcholine receptorsalkaloidepibatidinenicotinicABT 418α4β2α3β4Inhibitorinhibitorinhibit

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