Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine

Myrna Déciga-Campos, Gabriel Navarrete-Vázquez, Francisco Javier López-Muñoz, Tadeusz Librowski, Amanda Sánchez-Recillas, Victor Yañez-Pérez, Rolffy Ortiz-Andrade

Research output: Contribution to journalArticle

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Abstract

© 2016 Elsevier Inc. All rights reserved. Aim N-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA), a lidocaine analogue, has potential applications in treating neuropathic pain. The aim of this work was to characterize the pharmacological activity of LIA related with central nervous system and cardiovascular activity. Methods Anesthetic effect was tested in Guinea pigs and mice. Ambulatory activity, anti-anxiety effect, sodium pentobarbital (PB)-induced hypnosis and pentylenetetrazol (PTZ)-induced seizures test were evaluated in mice to determine the possible central nervous system activity. The cardiovascular activities in vivo and ex vivo were analyzed in rats. Key findings LIA (2%) presents, similar to lidocaine (2%), anesthetic activity on the corneal reflex, infiltration anesthesia and tail immersion test. LIA (1-100 mg/kg, i.p.), similar to lidocaine (1-100 mg/kg, i.p.)resents a dose-dependent sedative-hypnotic effect in mice. Both compounds did not produce anti-anxiety activity in mice. LIA did not prevent PTZ-induced seizures. However, LIA itself did not produce seizures at high doses in mice, as lidocaine does. LIA is a vasorelaxant compound for smooth muscle cells and presents hypotensive effect in vivo without increments to the heart rate significantly. Significance High doses of lidocaine produce seizures and vasoconstriction. In this study, we found that LIA shares a similar pharmacological profile as lidocaine's but without the primary adverse effects of seizures and vasoconstriction.
Original languageAmerican English
Pages (from-to)48-55
Number of pages42
JournalLife Sciences
DOIs
StatePublished - 15 Jun 2016

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Lidocaine
Pharmacology
Seizures
Pentylenetetrazole
Neurology
Vasoconstriction
Hypnotics and Sedatives
Anesthetics
Central Nervous System
Blinking
Hypnosis
Anti-Anxiety Agents
Neuralgia
Immersion
Pentobarbital
Local Anesthesia
Vasodilator Agents
Infiltration
Smooth Muscle Myocytes
Muscle

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Déciga-Campos, M., Navarrete-Vázquez, G., López-Muñoz, F. J., Librowski, T., Sánchez-Recillas, A., Yañez-Pérez, V., & Ortiz-Andrade, R. (2016). Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine. Life Sciences, 48-55. https://doi.org/10.1016/j.lfs.2016.05.015
Déciga-Campos, Myrna ; Navarrete-Vázquez, Gabriel ; López-Muñoz, Francisco Javier ; Librowski, Tadeusz ; Sánchez-Recillas, Amanda ; Yañez-Pérez, Victor ; Ortiz-Andrade, Rolffy. / Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine. In: Life Sciences. 2016 ; pp. 48-55.
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abstract = "{\circledC} 2016 Elsevier Inc. All rights reserved. Aim N-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA), a lidocaine analogue, has potential applications in treating neuropathic pain. The aim of this work was to characterize the pharmacological activity of LIA related with central nervous system and cardiovascular activity. Methods Anesthetic effect was tested in Guinea pigs and mice. Ambulatory activity, anti-anxiety effect, sodium pentobarbital (PB)-induced hypnosis and pentylenetetrazol (PTZ)-induced seizures test were evaluated in mice to determine the possible central nervous system activity. The cardiovascular activities in vivo and ex vivo were analyzed in rats. Key findings LIA (2{\%}) presents, similar to lidocaine (2{\%}), anesthetic activity on the corneal reflex, infiltration anesthesia and tail immersion test. LIA (1-100 mg/kg, i.p.), similar to lidocaine (1-100 mg/kg, i.p.)resents a dose-dependent sedative-hypnotic effect in mice. Both compounds did not produce anti-anxiety activity in mice. LIA did not prevent PTZ-induced seizures. However, LIA itself did not produce seizures at high doses in mice, as lidocaine does. LIA is a vasorelaxant compound for smooth muscle cells and presents hypotensive effect in vivo without increments to the heart rate significantly. Significance High doses of lidocaine produce seizures and vasoconstriction. In this study, we found that LIA shares a similar pharmacological profile as lidocaine's but without the primary adverse effects of seizures and vasoconstriction.",
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Déciga-Campos, M, Navarrete-Vázquez, G, López-Muñoz, FJ, Librowski, T, Sánchez-Recillas, A, Yañez-Pérez, V & Ortiz-Andrade, R 2016, 'Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine', Life Sciences, pp. 48-55. https://doi.org/10.1016/j.lfs.2016.05.015

Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine. / Déciga-Campos, Myrna; Navarrete-Vázquez, Gabriel; López-Muñoz, Francisco Javier; Librowski, Tadeusz; Sánchez-Recillas, Amanda; Yañez-Pérez, Victor; Ortiz-Andrade, Rolffy.

In: Life Sciences, 15.06.2016, p. 48-55.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine

AU - Déciga-Campos, Myrna

AU - Navarrete-Vázquez, Gabriel

AU - López-Muñoz, Francisco Javier

AU - Librowski, Tadeusz

AU - Sánchez-Recillas, Amanda

AU - Yañez-Pérez, Victor

AU - Ortiz-Andrade, Rolffy

PY - 2016/6/15

Y1 - 2016/6/15

N2 - © 2016 Elsevier Inc. All rights reserved. Aim N-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA), a lidocaine analogue, has potential applications in treating neuropathic pain. The aim of this work was to characterize the pharmacological activity of LIA related with central nervous system and cardiovascular activity. Methods Anesthetic effect was tested in Guinea pigs and mice. Ambulatory activity, anti-anxiety effect, sodium pentobarbital (PB)-induced hypnosis and pentylenetetrazol (PTZ)-induced seizures test were evaluated in mice to determine the possible central nervous system activity. The cardiovascular activities in vivo and ex vivo were analyzed in rats. Key findings LIA (2%) presents, similar to lidocaine (2%), anesthetic activity on the corneal reflex, infiltration anesthesia and tail immersion test. LIA (1-100 mg/kg, i.p.), similar to lidocaine (1-100 mg/kg, i.p.)resents a dose-dependent sedative-hypnotic effect in mice. Both compounds did not produce anti-anxiety activity in mice. LIA did not prevent PTZ-induced seizures. However, LIA itself did not produce seizures at high doses in mice, as lidocaine does. LIA is a vasorelaxant compound for smooth muscle cells and presents hypotensive effect in vivo without increments to the heart rate significantly. Significance High doses of lidocaine produce seizures and vasoconstriction. In this study, we found that LIA shares a similar pharmacological profile as lidocaine's but without the primary adverse effects of seizures and vasoconstriction.

AB - © 2016 Elsevier Inc. All rights reserved. Aim N-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA), a lidocaine analogue, has potential applications in treating neuropathic pain. The aim of this work was to characterize the pharmacological activity of LIA related with central nervous system and cardiovascular activity. Methods Anesthetic effect was tested in Guinea pigs and mice. Ambulatory activity, anti-anxiety effect, sodium pentobarbital (PB)-induced hypnosis and pentylenetetrazol (PTZ)-induced seizures test were evaluated in mice to determine the possible central nervous system activity. The cardiovascular activities in vivo and ex vivo were analyzed in rats. Key findings LIA (2%) presents, similar to lidocaine (2%), anesthetic activity on the corneal reflex, infiltration anesthesia and tail immersion test. LIA (1-100 mg/kg, i.p.), similar to lidocaine (1-100 mg/kg, i.p.)resents a dose-dependent sedative-hypnotic effect in mice. Both compounds did not produce anti-anxiety activity in mice. LIA did not prevent PTZ-induced seizures. However, LIA itself did not produce seizures at high doses in mice, as lidocaine does. LIA is a vasorelaxant compound for smooth muscle cells and presents hypotensive effect in vivo without increments to the heart rate significantly. Significance High doses of lidocaine produce seizures and vasoconstriction. In this study, we found that LIA shares a similar pharmacological profile as lidocaine's but without the primary adverse effects of seizures and vasoconstriction.

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