| Identification | Back Directory | [Name]
EPIBOXIDINE HCL | [CAS]
188895-96-7 | [Synonyms]
EPIBOXIDINE HCL
(+-)-epiboxidine
exo-7-azabicyclo(2.2.1)heptan
EPIBOXIDINE HYDROCHLORIDE \ POTENT NICOT
5-[(1S,3S,4R)-7-azabicyclo[2.2.1]heptan-3-yl]-3-methyl-1,2-oxazole
7-Azabicyclo[2.2.1]heptane, 2-(3-methyl-5-isoxazolyl)-, (1R,2S,4S)-rel- | [Molecular Formula]
C10H14N2O | [MDL Number]
MFCD01321042 | [MOL File]
188895-96-7.mol | [Molecular Weight]
178.23 |
| Chemical Properties | Back Directory | [Melting point ]
200-205 °C (decomp) | [Boiling point ]
313.1±27.0 °C(Predicted) | [density ]
1.130±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
H2O: 22 mg/mL | [pka]
10.14±0.40(Predicted) | [color ]
yellow | [Water Solubility ]
H2O: 22mg/mL |
| Hazard Information | Back Directory | [Uses]
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]. | [Biochem/physiol Actions]
Potent nicotinic acetylcholine receptor agonist; analog of epibatidine | [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]. | 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.
|
| [References]
[1] Fitch RW, et al. Homoepiboxidines: further potent agonists for nicotinic receptors. Bioorg Med Chem. 2004;12(1):179-190. DOI:10.1016/j.bmc.2003.10.015
[2] Badio B, et al. Synthesis and nicotinic activity of epiboxidine: an isoxazole analogue of epibatidine. Eur J Pharmacol. 1997;321(2):189-194. DOI:10.1016/s0014-2999(96)00939-9 |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
| Company Name: |
SIGMA-RBI
|
| Tel: |
800 736 3690 (Orders) |
| Website: |
www.sigma-aldrich.com |
|