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14 results on '"Cobos, E J"'

11. Bupivacaine-induced cellular entry of QX-314 and its contribution to differential nerve block

Author

Brenneis, C, primary, Kistner, K, additional, Puopolo, M, additional, Jo, S, additional, Roberson, DP, additional, Sisignano, M, additional, Segal, D, additional, Cobos, E J, additional, Wainger, B J, additional, Labocha, S, additional, Ferreirós, N, additional, von Hehn, C, additional, Tran, J, additional, Geisslinger, G, additional, Reeh, P W, additional, Bean, B P, additional, and Woolf, C J, additional

Published
2013
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12. 5,6-EET Is Released upon Neuronal Activity and Induces Mechanical Pain Hypersensitivity via TRPA1 on Central Afferent Terminals

Author

Sisignano, M., primary, Park, C.-K., additional, Angioni, C., additional, Zhang, D. D., additional, von Hehn, C., additional, Cobos, E. J., additional, Ghasemlou, N., additional, Xu, Z.-Z., additional, Kumaran, V., additional, Lu, R., additional, Grant, A., additional, Fischer, M. J. M., additional, Schmidtko, A., additional, Reeh, P., additional, Ji, R.-R., additional, Woolf, C. J., additional, Geisslinger, G., additional, Scholich, K., additional, and Brenneis, C., additional

Published
2012
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13. Sigma-1 Receptor Agonism Promotes Mechanical Allodynia After Priming the Nociceptive System with Capsaicin

Author

José M. Baeyens, Rafael González-Cano, Cristina Sánchez-Fernández, Sandra Yeste, Francisco R. Nieto, José Manuel Entrena, Enrique J. Cobos, [Entrena, J. M.] Univ Granada, Inst Neurosci, Biomed Res Ctr, Granada 18100, Spain, [Sanchez-Fernandez, C.] Univ Granada, Inst Neurosci, Biomed Res Ctr, Granada 18100, Spain, [Nieto, F. R.] Univ Granada, Inst Neurosci, Biomed Res Ctr, Granada 18100, Spain, [Gonzalez-Cano, R.] Univ Granada, Inst Neurosci, Biomed Res Ctr, Granada 18100, Spain, [Cobos, E. J.] Univ Granada, Inst Neurosci, Biomed Res Ctr, Granada 18100, Spain, [Baeyens, J. M.] Univ Granada, Inst Neurosci, Biomed Res Ctr, Granada 18100, Spain, [Entrena, J. M.] Univ Granada, Sci Instrumentat Ctr, Anim Behav Res Unit, Granada 18100, Spain, [Entrena, J. M.] Univ Hosp Complex Granada, Biosanitary Res Inst, Granada 18012, Spain, [Sanchez-Fernandez, C.] Univ Hosp Complex Granada, Biosanitary Res Inst, Granada 18012, Spain, [Nieto, F. R.] Univ Hosp Complex Granada, Biosanitary Res Inst, Granada 18012, Spain, [Gonzalez-Cano, R.] Univ Hosp Complex Granada, Biosanitary Res Inst, Granada 18012, Spain, [Cobos, E. J.] Univ Hosp Complex Granada, Biosanitary Res Inst, Granada 18012, Spain, [Baeyens, J. M.] Univ Hosp Complex Granada, Biosanitary Res Inst, Granada 18012, Spain, [Sanchez-Fernandez, C.] Univ Granada, Sch Med, Dept Pharmacol, Granada 18016, Spain, [Nieto, F. R.] Univ Granada, Sch Med, Dept Pharmacol, Granada 18016, Spain, [Gonzalez-Cano, R.] Univ Granada, Sch Med, Dept Pharmacol, Granada 18016, Spain, [Cobos, E. J.] Univ Granada, Sch Med, Dept Pharmacol, Granada 18016, Spain, [Baeyens, J. M.] Univ Granada, Sch Med, Dept Pharmacol, Granada 18016, Spain, [Yeste, S.] Drug Discovery & Preclin Dev, Barcelona, Spain, [Cobos, E. J.] Teofilo Hernando Inst Drug Discovery, Madrid 28029, Spain, FPU grants from Spanish Ministerio de Educacion y Ciencia (MEC), postdoctoral Juan de la Cierva grant (Spanish goverment), and Research Program of the University of Granada

Subjects
0301 basic medicine, Agonist, Male, Nociception, Pain Threshold, Pentazocine, medicine.drug_class, Receptor expression, Morpholines, Expression, Chaperone, Cyclopentanes, Pharmacology, Neuropathic pain, Article, Induction, 03 medical and health sciences, chemistry.chemical_compound, Mice, 0302 clinical medicine, Threshold of pain, medicine, Hypersensitivity, Animals, Receptors, sigma, Phosphorylation, Pain Measurement, Multidisciplinary, Sigma-1 receptor, fungi, Mice role, Disease Models, Animal, 030104 developmental biology, chemistry, Liver, Capsaicin, Hyperalgesia, Anesthesia, Haloperidol, bacteria, Antagonists, medicine.symptom, 030217 neurology & neurosurgery, medicine.drug
Abstract

Sigma-1 receptor antagonists promote antinociception in several models of pain, but the effects of sigma-1 agonists on nociception (particularly when the nociceptive system is primed) are not so well characterized; therefore we evaluated the effects of sigma-1 agonists on pain under different experimental conditions. The systemic administration of the selective sigma-1 agonists (+)-pentazocine and PRE-084, as well as the nonselective sigma-1 agonist carbetapentane (used clinically as an antitussive drug), did not alter sensitivity to mechanical stimulation under baseline conditions. However, they greatly promoted secondary mechanical allodynia after priming the nociceptive system with capsaicin. These effects of sigma-1 agonists were consistent in terms potency with the affinities of these drugs for sigma-1 receptors, were reversed by sigma-1 antagonists, and were not observed in sigma-1 knockout mice, indicating that they are sigma-1-mediated. Repeated systemic treatment with PRE-084 induced proallodynic effects even 24 h after treatment completion, but only after the nociceptive system was primed. However, neither the presence of this drug in the organism nor changes in sigma-1 receptor expression in areas involved in pain processing explains its long-term effects, suggesting that sustained sigma-1 agonism induces plastic changes in the nociceptive system that promote nociception.

Published
2016
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14. (+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/σ 1 antagonist properties and antinociceptive effects.

Author

Prezzavento O, Arena E, Sánchez-Fernández C, Turnaturi R, Parenti C, Marrazzo A, Catalano R, Amata E, Pasquinucci L, and Cobos EJ

Subjects
Analgesics chemical synthesis, Analgesics chemistry, Analgesics pharmacology, Animals, Binding Sites, Mice, Molecular Structure, Morpholines chemistry, Morpholines pharmacology, Narcotic Antagonists chemistry, Pain drug therapy, Pain Measurement, Phenazocine chemistry, Protein Binding drug effects, Stereoisomerism, Narcotic Antagonists chemical synthesis, Narcotic Antagonists pharmacology, Phenazocine chemical synthesis, Phenazocine pharmacology, Receptors, Opioid agonists
Abstract

cis-N-Substituted N-normetazocine enantiomers possess peculiar pharmacological profiles. Indeed, dextro enantiomers bind with high affinity σ 1 receptor while opposite enantiomers bind opioid receptors. In spite of their stereochemistry, cis-N-2-phenylethyl N-normetazocine (phenazocine) enantiomers showed mixed opioid/σ 1 receptor profiles and a significant in vivo analgesia. To the best of our knowledge, there is no information available regarding the evaluation of σ 1 pharmacological profile in the antinociceptive effects of (+)- and (-)-phenazocine. Therefore, the present study was designed to ascertain this component by in vitro and in vivo studies. In particular, we tested the σ 1 affinity of both enantiomers by a predictive binding assay in absence or presence of phenytoin (DPH). Our results showed that DPH (1 mM) did not increase the σ 1 receptor affinity of (+)-and (-)-phenazocine (K i  = 3.8 ± 0.4 nM, K i  = 85 ± 2.0 nM, respectively) suggesting a σ 1 antagonist profile of both enantiomers. This σ 1 antagonistic component of two phenazocine enantiomers was corroborated by in vivo studies in which the selective σ 1 receptor agonist PRE-084, was able to unmask their σ 1 antagonistic component associated with the opioid activity. The σ 1 antagonistic component of (+)- and (-)-phenazocine may justify their analgesic activity and it suggests that they may constitute useful lead compounds to develop new ligands with this dual activity., (Copyright © 2016 Elsevier Masson SAS. All rights reserved.)

Published
2017
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