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Molecules 2017, 22(5), 800; doi:10.3390/molecules22050800

The Hypnotic, Anxiolytic, and Antinociceptive Profile of a Novel µ-Opioid Agonist

1
Programa de Pesquisa em Desenvolvimento de Fármacos, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro RJ 21941-902, Brazil
2
Instituto de Química, Universidade Federal do Rio de Janeiro, Rio de Janeiro RJ 21941-909, Brazil
3
Instituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR), Rio de Janeiro RJ 21941-971, Brazil
4
Instituto de Química, Universidade Federal Fluminense, Niterói RJ 24020-150, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 10 March 2017 / Revised: 17 April 2017 / Accepted: 26 April 2017 / Published: 16 May 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [2044 KB, uploaded 16 May 2017]   |  

Abstract

5′-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 112 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 µmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a µ-opioid antagonist. Locomotor and motor activities were not affected by PILAB 8. The anxiolytic effect of PILAB 8 was evaluated next in an elevated-plus maze apparatus. PILAB 8 and midazolam increased a percentage of entries and spent time in the open arms of the apparatus compared with the control group. Conversely, a decrease in the percentages of entries and time spent in the closed arms were observed. Pretreatment with naloxone, a non-specific opioid antagonist, prior to administration of PILAB 8 exhibited a reverted anxiolytic effect. PILAB 8 exhibited antinociceptive activity in the hot plate test, and reduced reactivity to formalin in the neurogenic and the inflammatory phases. These data suggest that PILAB 8 can activate µ-opioid receptors to provoke antinociceptive and anti-inflammatory effects in mice. View Full-Text
Keywords: novel µ-opioid agonist; hypnosis; antinociception; anti-inflammatory effect; mice novel µ-opioid agonist; hypnosis; antinociception; anti-inflammatory effect; mice
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MDPI and ACS Style

Montes, G.C.; da Silva, B.N.M.; Rezende, B.; Sudo, R.T.; Ferreira, V.F.; de Carvalho da Silva, F.; da Cunha Pinto, A.; da Silva, B.V.; Zapata-Sudo, G. The Hypnotic, Anxiolytic, and Antinociceptive Profile of a Novel µ-Opioid Agonist. Molecules 2017, 22, 800.

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