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Epibatidine: a novel (chloropyridyl)azabicycloheptane with potent analgesic activity from an ecuadoran poison frog

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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 alkaloids

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Evidence for the tonic inhibition of spinal pain by nicotinic cholinergic transmission through primary afferents

TL;DR: These findings suggest that primary afferent cholinergic neurons produce tonic inhibition of spinal pain through nAChR activation, and that intrathecal administration of nicotine rescues the loss of tonic cholinergy inhibition.
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The analgesic effect of epibatidine and isomers

TL;DR: The racemic form, d, and l-enantiomers and the 7-N-methyl derivative of synthetic epibatidine are equally potent in the tail-flick analgesic model without any enantioselectivity and the analgesic response is not antagonized by pretreatment with naloxone.
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Microbial Pyrrolnitrin: Natural Metabolite with Immense Practical Utility.

TL;DR: Pyrrolnitrin (PRN) is a microbial pyrrole halometabolite of immense antimicrobial significance for agricultural, pharmaceutical and industrial implications as mentioned in this paper, which has been isolated from rhizospheric fluorescent or non-fluorescent pseudomonads, Serratia and Burkholderia.
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Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.

TL;DR: The results suggest that these compounds will be highly useful for identifying which specific receptor subtypes are involved in each of nicotine's pharmacological effects and deserve consideration as potential pharmacotherapies for treatment of smoking cessation.
Journal ArticleDOI

Alpha 4 nicotinic acetylcholine receptor subunit links cholinergic to brainstem monoaminergic neurotransmission

TL;DR: Results suggest that the α4 subunit is positioned to mediate the effects of acetylcholine widely across many, if not all, monoaminergic neurons in the brainstem, and suggest that even selective α4 ligand may have widespread effects on brain monoamine neurotransmission.
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