Literature DB >> 8112391

Epibatidine is a nicotinic analgesic.

C Qian1, T Li, T Y Shen, L Libertine-Garahan, J Eckman, T Biftu, S Ip.   

Abstract

Epibatidine, an alkaloid isolated from skin of the poison frog, Epipedobates tricolor, has been shown to be a very potent analgesic with a non-opioid mechanism of action. We found that epibatidine was about 120 times more potent and has longer duration than nicotine in analgesia, which could be antagonized by pretreatment with mecamylamine. Furthermore, epibatidine competed with high affinity (IC50 = 70 pM, Ki = 43 pM) for [3H]cytisine binding in rat brain preparations. These results indicated that the analgesic activity of epibatidine is attributed to its unique property as the most potent nicotinic acetylcholine receptor agonist.

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Year:  1993        PMID: 8112391     DOI: 10.1016/0014-2999(93)90043-h

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN: 0014-2999            Impact factor:   4.432


  8 in total

Review 1.  Nicotinic ACh receptors as therapeutic targets in CNS disorders.

Authors:  Kelly T Dineley; Anshul A Pandya; Jerrel L Yakel
Journal:  Trends Pharmacol Sci       Date:  2015-01-29       Impact factor: 14.819

2.  Functional neurochemical evidence for the presence of presynaptic nicotinic acetylcholine receptors at the terminal region of myenteric motoneurons: a study with epibatidine.

Authors:  P Mandl; J P Kiss; E S Vizi
Journal:  Neurochem Res       Date:  2003-04       Impact factor: 3.996

Review 3.  The therapeutic promise of positive allosteric modulation of nicotinic receptors.

Authors:  Victor V Uteshev
Journal:  Eur J Pharmacol       Date:  2014-02-12       Impact factor: 4.432

4.  Antinociceptive and toxic effects of (+)-epibatidine oxalate attributable to nicotinic agonist activity.

Authors:  N M Rupniak; S Patel; R Marwood; J Webb; J R Traynor; J Elliott; S B Freedman; S R Fletcher; R G Hill
Journal:  Br J Pharmacol       Date:  1994-12       Impact factor: 8.739

5.  Nanoparticle-conjugated animal venom-toxins and their possible therapeutic potential.

Authors:  Archita Biswas; Aparna Gomes; Jayeeta Sengupta; Poulami Datta; Santiswarup Singha; Anjan Kr Dasgupta; Antony Gomes
Journal:  J Venom Res       Date:  2012-10-23

Review 6.  Epibatidine: A Promising Natural Alkaloid in Health.

Authors:  Bahare Salehi; Simona Sestito; Simona Rapposelli; Gregorio Peron; Daniela Calina; Mehdi Sharifi-Rad; Farukh Sharopov; Natália Martins; Javad Sharifi-Rad
Journal:  Biomolecules       Date:  2018-12-23

7.  The activation of nicotinic acetylcholine receptors enhances the inhibitory synaptic transmission in the deep dorsal horn neurons of the adult rat spinal cord.

Authors:  Daisuke Takeda; Terumasa Nakatsuka; Jianguo G Gu; Munehito Yoshida
Journal:  Mol Pain       Date:  2007-09-25       Impact factor: 3.395

Review 8.  Pyridine alkaloids with activity in the central nervous system.

Authors:  Simon X Lin; Maurice A Curtis; Jonathan Sperry
Journal:  Bioorg Med Chem       Date:  2020-10-16       Impact factor: 3.641

  8 in total

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