Journal ArticleDOI
Epibatidine: a novel (chloropyridyl)azabicycloheptane with potent analgesic activity from an ecuadoran poison frog
Thomas F. Spande,H. M. Garraffo,M. W. Edwards,Herman J. C. Yeh,Lewis K. Pannell,John W. Daly +5 more
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TLDR
A potent non-opioid analgesic, epibatidine, has been isolated from skins of the Ecuadoran poison frog, Epipedobates tricolor, and its structure determined by MS, IR, and 1 H NMR analyses as exo-2-(6-chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane represents a unique new class of alkaloids.Abstract:
A potent non-opioid analgesic, epibatidine, has been isolated from skins of the Ecuadoran poison frog, Epipedobates tricolor, and its structure determined by MS, IR, and 1 H NMR analyses as exo-2-(6-chloro-3-pyridyl)-7-azabicyclo[2.2.1]heptane. It represents a unique new class of alkaloidsread more
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Targeting the cholinergic system as a therapeutic strategy for the treatment of pain.
Philip G. Jones,John Dunlop +1 more
TL;DR: The evidence for the therapeutic exploitation of the cholinergic system as an approach to treat pain is examined and the evidence for a broad therapeutic potential is discussed.
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Tonic nicotinic modulation of serotoninergic transmission in the spinal cord.
TL;DR: The presence of a tonic nicotinic modulation of 5-HT release indicates that endogenous acetylcholine plays a role in the physiological regulation of descending 5- HT pathways to the spinal cord.
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Evaluation of anti-nociceptive effects of neuronal nicotinic acetylcholine receptor (NAChR) ligands in the rat tail-flick assay.
TL;DR: Anti-nociceptive effects of neuronal nicotinic acetylcholine receptor (NAChR) ligands were evaluated and indicated that a sub-population of NAChR receptors are located pre-synaptically on noradrenergic and/or serotoninergic pathways in the hippocampus, indicating a minimal role for these receptors in the tail-flick response.
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Pharmacological effects of epibatidine optical enantiomers
TL;DR: There was no significant enantioselectivity for these effects in the authors' study, and the discriminative effect of L- and D-epibatidine in rats was blocked by mecamylamine but not by hexamethonium.
Journal ArticleDOI
A versatile total synthesis of epibatidine and analogs
Dao Fei Huang,T.Y Shen +1 more
TL;DR: A racemic mixture of epibatidine, a potent analgesic alkaloid possessing a 7-azanorbornane structure, has been synthesized via a versatile four-step synthetic route as mentioned in this paper.