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Epiboxidine is a chemical compound which acts as a partial agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. It was developed as a less toxic analogue of the potent frog-derived alkaloid epibatidine, which is around 200 times stronger than morphine as an analgesic but produces extremely dangerous toxic nicotinic side effects. Epiboxidine is around one-tenth as potent as epibatidine as an α4β2 agonist, but has around the same potency as an α3β4 agonist. It has only one-tenth of the analgesic power of epibatidine, but is also much less toxic.

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rdf:type
rdfs:label
  • Epiboxidina (es)
  • Epiboxidine (en)
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  • Epiboxidine is a chemical compound which acts as a partial agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. It was developed as a less toxic analogue of the potent frog-derived alkaloid epibatidine, which is around 200 times stronger than morphine as an analgesic but produces extremely dangerous toxic nicotinic side effects. Epiboxidine is around one-tenth as potent as epibatidine as an α4β2 agonist, but has around the same potency as an α3β4 agonist. It has only one-tenth of the analgesic power of epibatidine, but is also much less toxic. (en)
  • La epiboxidina es un compuesto químico heterocíclico que se comporta como un potente agonista parcial de los receptores nicotínicos​ que combina las subestructuras de la epibatidina y del ABT-418.Actúa como un agonista parcial de los receptores nicotínicos de la acetilcolina, uniéndose a α3β4 y a los subtipos α4β2. Fue desarrollado como un análogo menos tóxico que la epibatidina (potente alcaloide extraído de la rana que es de alrededor de 200 veces más fuerte que la morfina como analgésico). Aunque tiene sólo una décima parte de la potencia analgésica como agonista α4β2 que la epibatidina, tiene alrededor de la misma potencia que un agonista α3β4 que esta y es mucho menos tóxica.Este producto es comercial y lo podemos comprar por ejemplo en Santa Cruz Biotechnology. (es)
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  • http://commons.wikimedia.org/wiki/Special:FilePath/Epiboxidine_skeletal.svg
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  • Investigational (en)
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PubChem
SMILES
  • CC1=NOC[C@H]2C[C@@H]3CC[C@H]2N3 (en)
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StdInChIKey
  • GEEFPQBPVBFCSD-XHNCKOQMSA-N (en)
UNII
  • XI646L2ARJ (en)
has abstract
  • Epiboxidine is a chemical compound which acts as a partial agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. It was developed as a less toxic analogue of the potent frog-derived alkaloid epibatidine, which is around 200 times stronger than morphine as an analgesic but produces extremely dangerous toxic nicotinic side effects. Epiboxidine is around one-tenth as potent as epibatidine as an α4β2 agonist, but has around the same potency as an α3β4 agonist. It has only one-tenth of the analgesic power of epibatidine, but is also much less toxic. (en)
  • La epiboxidina es un compuesto químico heterocíclico que se comporta como un potente agonista parcial de los receptores nicotínicos​ que combina las subestructuras de la epibatidina y del ABT-418.Actúa como un agonista parcial de los receptores nicotínicos de la acetilcolina, uniéndose a α3β4 y a los subtipos α4β2. Fue desarrollado como un análogo menos tóxico que la epibatidina (potente alcaloide extraído de la rana que es de alrededor de 200 veces más fuerte que la morfina como analgésico). Aunque tiene sólo una décima parte de la potencia analgésica como agonista α4β2 que la epibatidina, tiene alrededor de la misma potencia que un agonista α3β4 que esta y es mucho menos tóxica.Este producto es comercial y lo podemos comprar por ejemplo en Santa Cruz Biotechnology. (es)
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CAS number
  • 188895-96-7
FDA UNII code
  • XI646L2ARJ
PubChem
  • 5747670
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