Next Article in Journal
Modes of Cell Death Induced by Photodynamic Therapy Using Zinc Phthalocyanine in Lung Cancer Cells Grown as a Monolayer and Three-Dimensional Multicellular Spheroids
Previous Article in Journal
The Phenolic Fraction of Mentha haplocalyx and Its Constituent Linarin Ameliorate Inflammatory Response through Inactivation of NF-κB and MAPKs in Lipopolysaccharide-Induced RAW264.7 Cells
Article Menu
Issue 5 (May) cover image

Export Article

Open AccessArticle
Molecules 2017, 22(5), 800;

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

Programa de Pesquisa em Desenvolvimento de Fármacos, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro RJ 21941-902, Brazil
Instituto de Química, Universidade Federal do Rio de Janeiro, Rio de Janeiro RJ 21941-909, Brazil
Instituto Nacional de Ciência e Tecnologia de Fármacos e Medicamentos (INCT-INOFAR), Rio de Janeiro RJ 21941-971, Brazil
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)
Full-Text   |   PDF [2044 KB, uploaded 16 May 2017]   |  


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

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material


Share & Cite This Article

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top