E1145
(±)-Epibatidine dihydrochloride hydrate
≥98% (HPLC), powder
Sinonimo/i:
exo-(±)-2-(6-Chloro-3-pyridinyl)-7-azabicyclo[2.2.1]heptane dihydrochloride hydrate
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5 MG
288,00 €
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5 MG
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About This Item
Formula empirica (notazione di Hill):
C11H13ClN2 · 2HCl · xH2O
Peso molecolare:
281.61 (anhydrous basis)
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77
Prodotti consigliati
Livello qualitativo
Saggio
≥98% (HPLC)
Stato
powder
Condizioni di stoccaggio
desiccated
Colore
off-white
Solubilità
DMSO: >4 mg/mL
methanol: 4 mg/mL
Stringa SMILE
Cl[H].Cl[H].[H]O[H].Clc1ccc(cn1)[C@H]2CC3CCC2N3
InChI
1S/C11H13ClN2.2ClH.H2O/c12-11-4-1-7(6-13-11)9-5-8-2-3-10(9)14-8;;;/h1,4,6,8-10,14H,2-3,5H2;2*1H;1H2/t8?,9-,10?;;;/m1.../s1
AXWYRFKDLRSESC-VAGRNHIFSA-N
Azioni biochim/fisiol
Epibatidine is most potent nicotinic acetylcholine receptor agonist known; non-opioid analgesic.
The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in the guinea-pig ileum (contraction mediated by the cholinergic neurons of the ileum) and in pithed and atropinized rats (rise in blood pressure). Epibatidine also activated nicotinic receptors at the peripheral terminals of afferent C-fibres (rabbit ear) and in the brain (antidiuresis in rats). The agonistic effects of epibatidine were followed by long-lasting receptor desensitization. No antinociceptive effect of epibatidine was seen in rats at a dose free of motor impairment. On muscle end plate nicotinic receptors of the rat diaphragm (not responding to depolarizing agents by contraction), epibatidine was equipotent with suxamethonium in causing neuromuscular inhibition. On an extraocular muscle of the rabbit (responding to depolarizing agents by contraction) epibatidine in vitro and in situ caused a contraction at a 100-fold lower dose than suxamethonium. The Straub tail reaction in mice to epibatidine could be attributed to the sustained stimulation of motor end plate receptors of the "slow contracting" type of muscle fibres by epibatidine. Epibatidine was the most potent agonist on all neuronal and neuromuscular nicotinic receptors examined.
Caratteristiche e vantaggi
This compound is featured on the Acetylcholine Receptors (Nicotinic) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Avvertenze
Danger
Indicazioni di pericolo
Consigli di prudenza
Classi di pericolo
Acute Tox. 2 Dermal - Acute Tox. 2 Oral
Codice della classe di stoccaggio
6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
Classe di pericolosità dell'acqua (WGK)
WGK 3
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
Dispositivi di protezione individuale
Eyeshields, Faceshields, Gloves, type P3 (EN 143) respirator cartridges
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I documenti relativi ai prodotti acquistati recentemente sono disponibili nell’Archivio dei documenti.
Aurora Alvarez-Buylla et al.
eLife, 12 (2024-01-11)
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Naunyn-Schmiedeberg's archives of pharmacology, 359(5), 378-385 (1999-09-25)
The activity of epibatidine at neuronal and neuromuscular nicotinic acetylcholine receptors was investigated in several in situ and in vitro systems and compared with the activity of nicotine and suxamethonium. Activation of ganglionic nicotinic receptors by epibatidine was shown in
Ali Yehia et al.
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W Sihver et al.
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The laminar binding distribution of three nicotinic receptor agonists, [3H](-)nicotine, [3H]cytisine, and [3H]epibatidine, and their relation to the [3H]vesamicol binding, which is known to represent the vesicular acetylcholine transport sites, was performed employing in vitro autoradiography on the medial temporal
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