title: Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analogue of lidocaine.
abstract: OBJECTIVE
  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.
  
  
  RESULTS
  LIA (2%) presents, similar to lidocaine (2%), anesthetic activity on the corneal reflex, infiltration anesthesia and tail immersion test. LIA (1-100mg/kg, i.p.), similar to lidocaine (1-100mg/kg, i.p.), presents 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Sección de Estudios de Posgrado e Investigación de la Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de México, México. Electronic address: myrnadeciga@hotmail.com.
authors.forename: Myrna
authors.initials: M
authors.lastname: Déciga-Campos
authors.affiliation: Facultad de Farmacia de la Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos, México.
authors.forename: Gabriel
authors.initials: G
authors.lastname: Navarrete-Vázquez
authors.affiliation: Departamento de Farmacobiología, CINVESTAV-Sede Sur, Ciudad de México, México.
authors.forename: Francisco Javier
authors.initials: FJ
authors.lastname: López-Muñoz
authors.affiliation: Departament of Pharmacodynamics, Medical College, Jagiellonian University, Medyczna 9, 30-688 Kraków, Poland.
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Librowski
authors.affiliation: Laboratorio de Farmacología, Facultad de Química, Universidad Autónoma de Yucatán.
authors.forename: Amanda
authors.initials: A
authors.lastname: Sánchez-Recillas
authors.affiliation: Laboratorio de Farmacología, Facultad de Química, Universidad Autónoma de Yucatán.
authors.forename: Victor
authors.initials: V
authors.lastname: Yañez-Pérez
authors.affiliation: Laboratorio de Farmacología, Facultad de Química, Universidad Autónoma de Yucatán.
authors.forename: Rolffy
authors.initials: R
authors.lastname: Ortiz-Andrade
mesh_terms: D000779:Anesthetics, Local / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D002319:Cardiovascular System / Q000187:drug effects; D006168:Guinea Pigs; D006993:Hypnotics and Sedatives / Q000494:pharmacology; D008012:Lidocaine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D008297:Male; D051379:Mice; D010880:Piperidines / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar; D012640:Seizures / Q000139:chemically induced
chemical_list: D000779:Anesthetics, Local; D014151:Anti-Anxiety Agents; D006993:Hypnotics and Sedatives; C000614455:N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide; D010880:Piperidines; D008012:Lidocaine
keywords: Analogue of lidocaine; N-(2,6-Dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide; Pharmacological profile; Seizures