| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C10H14N2O |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Epiboxidine is a potent, selective agonist of neural nAChRs, with Ki values of 0.46 nM at rat α4β2 nAChRs and 1.2 nM at the human subtype. It is a methylisoxazole analog of the alkaloid Epibatidine and is also related to another nAChR agonist, ABT 418[1]. The compound has the molecular formula C10H14N2O and a molecular weight of 178.23 g/mol.
Physical & Chemical Properties
| CAS Number | 188895-96-7 |
|---|---|
| Molecular Formula | C10H14N2O |
| Molecular Weight | 178.23 g/mol |
| SMILES | CC1=NOC([C@@H]2[C@@H]3N[C@@H](CC3)C2)=C1 |
| Signaling Pathway | Membrane Transporter/Ion Channel; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
Ki: 0.46 nM (rat α4β2 nAChR) and 1.2 nM (human α4β2 nAChR)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
Epiboxidine shows affinity for, and functional activity at, α4β2 receptors in central neurons, with Kis of 0.46 and 1.2 in rat and human, respectively[1]. Epiboxidine is active at α3β4*-nicotinic receptors (ganglionic type) of PC12 cells (Ki of 19)[1]. Epiboxidine has much lower toxicity than Epibatidine[1]. In PC12 and TE671 cells, Epiboxidine stimulates sodium-22 influx, with EC50s of 0.18 and 2.6 μM[2].
In Vivo
Epiboxidine (20 μg/kg; ip; once) produces marked analgesic activity in mice[1]. Given once by intraperitoneal injection at 50 and 100 mg/kg, Epiboxidine causes marked antinociception in the hot-plate assay[2]. Epiboxidine blocks [3H]nicotine binding in rat cerebral cortical membranes with a Ki of 0.6 nM[2].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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