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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Short- and long-term enhancement of excitatory transmission in the spinal cord dorsal horn by nicotinic acetylcholine receptors
TL;DR: It is demonstrated that α7 nAChRs can contribute to both short- and long-term enhancement of glutamatergic synaptic transmission in the spinal cord dorsal horn and provide a possible mechanism for nicotinic hyperalgesia.
Journal ArticleDOI
Interacting amino acid replacements allow poison frogs to evolve epibatidine resistance.
Rebecca D. Tarvin,Cecilia M. Borghese,Wiebke Sachs,Wiebke Sachs,Juan C. Santos,Ying Lu,Lauren A. O’Connell,David C. Cannatella,R. Adron Harris,Harold H. Zakon +9 more
TL;DR: The results demonstrate how resistance to agonist toxins can evolve and that such genetic changes propel organisms toward an adaptive peak of chemical defense.
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Bicyclic proline analogues as organocatalysts for stereoselective aldol reactions: an in silico DFT study.
C. B. Shinisha,Raghavan B. Sunoj +1 more
TL;DR: Analysis of the transition state geometries revealed that the structural rigidity of catalysts, improved transition state organization as well as other weak interactions influence the relative stabilities of diastereomeric transition states and help contribute to the overall stereoselectivity in the aldol reaction.
Journal ArticleDOI
New molecules in analgesia
TL;DR: The prospects for new drug therapies based on the mitigation of some of the physiological and neurochemical changes that occur in the nociceptive pathway after injury are examined.