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Long‐lasting oral analgesic effects of N ‐protected aminophosphinic dual ENK ephalinase inhibitors ( DENKI s) in peripherally controlled pain

Autor: Xavier Nadal, Marie-Claude Fournie-Zaluski, Rafael Maldonado, Hervé Poras, Bernard P. Roques, Elisabeth Bonnard

Publikováno v: Pharmacology Research & Perspectives
Pharmacology Research & Perspectives, 2015, 3 (2), ⟨10.1002/prp2.116⟩
Recercat. Dipósit de la Recerca de Catalunya
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Pharmacology Research & Perspectives, Wiley, 2015, 3 (2), ⟨10.1002/prp2.116⟩

International audience; The peripheral endogenous opioid system is critically involved in neuropathic and inflammatory pain generation as suggested by the modulation of opioid receptors expression and enkephalins (ENKs) release observed in these pain

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b3eda526c7faf99255097198524e0ae
https://doi.org/10.1002/prp2.116

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First asymmetric synthesis of the Kelatorphan-like enkephalinase inhibitor (1S,2R,2 ' S)-2-[2 '-(N-hydroxycarbamoylmethyl)-3 '-phenylpropionylamino]cyclohexane-1-carboxylic acid

Autor: Stephen G. Davies, Darren J. Dixon

The first asymmetric synthesis of Kelatorphan-like enkephalinase inhibitor (1S,2R,2′S)-2-[2′-(N-hydroxycarbamoylmethyl)-3′- phenylpropionylamino]cyclohexane-1-carboxylic acid is achieved using lithium amide (R)-5 and pyrrolidinone auxiliary (R)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdd8e9a727bca57a5a28e2609a1a0847
https://doi.org/10.1039/a804660c

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Low doses of cyclic AMP-phosphodiesterase inhibitors rapidly evoke opioid receptor-mediated thermal hyperalgesia in naïve mice which is converted to prominent analgesia by cotreatment with ultra-low-dose naltrexone

Autor: Stanley M. Crain, Ke-Fei Shen

Publikováno v: Brain Research. 1231:16-24

Systemic (s.c.) injection in naive mice of cyclic AMP-phosphodiesterase (cAMP-PDE) inhibitors, e.g. 3-isobutyl-1-methylxanthine [(IBMX) or caffeine, 10 mg/kg] or the more specific cAMP-PDE inhibitor, rolipram (1 μg/kg), rapidly evokes thermal hypera

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::928c7ee93db23824e7b2c9541ca9f449
https://doi.org/10.1016/j.brainres.2008.07.015

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Akademický článek

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Inhibitors of Leukotriene A4 (LTA4) Hydrolase as Potential Anti-Inflammatory Agents>

Autor: Thomas D. Penning

Publikováno v: Current Pharmaceutical Design. 7:163-179

Leukotriene A4 (LTA4) hydrolase is a zinc-containing enzyme which stereospecifically catalyzes the hydrolysis of the epoxide LTA4 to the diol leukotriene B4 (LTB4). There is substantial evidence that LTB4 plays a significant role in the amplification

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fde0ffcee6eaf3fec9ce199d2e60d1d8
https://doi.org/10.2174/1381612013398248

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Kelatorphan and related analogs: potent and selective inhibitors of leukotriene A4 hydrolase

Autor: Gwen Grabowski Krivi, E.Yvonne Pyla, Stevan W. Djuric, Thomas D. Penning, Richard A. Haack, Leslie J Askonas, Stella S. Yu, Marshall L. Michener

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2517-2522

The hydroxamic acid-containing peptide kelatorphan, a known inhibitor of enkephalin-degrading enzymes, is a potent, non-competitive inhibitor of leukotriene A4 (LTA4) hydrolase. Analogs of kelatorphan were prepared and several significantly and selec

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f3a3f3d9ad1c6b8bb68f2906bec02974
https://doi.org/10.1016/0960-894x(95)00441-u

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Dopamine depletion augments endogenous opioid-induced locomotion in the nucleus accumbens using bothμ1 andδ opioid receptors

Autor: Peter W. Kalivas, Lynn Churchill, B.P. Roques

Publikováno v: Psychopharmacology. 120:347-355

The aim of this study is to analyze further the opioid receptor subtypes involved in the augmentation of behavioral activity after dopamine depletion in the nucleus accumbens of rats. Initially, the opioid receptors involved in the augmentation of lo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25c85f442b3f50fef2070c8e4801b0fb
https://doi.org/10.1007/bf02311183

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Effects of Phosphoramidon on Endothelin-1 and Big Endothelin-1 Production in Human Aortic Endothelial Cells

Autor: Yaeko Tsukahara, Yasuo Matsumura, Akiko Murakami, Kimi Takada, Takayo Kojima, Satoshi Murata, Masanori Takaoka, Shiro Morimoto

Publikováno v: Biological and Pharmaceutical Bulletin. 18:401-406

Using cultured human aortic endothelial cells, we examined the effects of phosphoramidon, an endothelin converting enzyme (ECE) inhibitor, on the release of endogenous endothelin-1 (ET-1) and big endothelin-1 (big ET-1), and on the generation of ET-1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14ec76ded0c28ade77ad59fa0a0c9187
https://doi.org/10.1248/bpb.18.401

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Antinociceptive effect of systemic kelatorphan, in mononeuropathic rats, involves different opioid receptor types

Autor: Valérie Kayser, Sun Hae Lee, Gisèle Guilbaud

Publikováno v: European Journal of Pharmacology. 264:61-67

The antinociceptive effect of i.v. kelatorphan (2.5, 5, 10 and 15 mg/kg), a mixed inhibitor of enkephalin degrading enzymes, was studied in a rat model of peripheral unilateral mononeuropathy (chronic constriction of the common sciatic nerve). Kelato

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5efea5b4852f7362682323ff80ed3950
https://doi.org/10.1016/0014-2999(94)90636-x

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