title: Antinociceptive Effect of 3-(2,3-Dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one in Mice Models of Induced Nociception.
abstract: The antinociceptive effects produced by intraperitoneal administration of a novel synthetic chalcone, 3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one (DMFP), were investigated in several mouse models of induced nociception. The administration of DMFP (0.1, 0.5, 1.0 and 5.0 mg/kg) produced significant attenuation on the acetic acid-induced abdominal-writhing test. It also produced a significant increase in response latency time in the hot-plate test and a marked reduction in time spent licking the injected paw in both phases of the formalin-induced paw-licking test. In addition, it was also demonstrated that DMFP exhibited significant inhibition of the neurogenic nociceptive response induced by intraplantar injections of capsaicin and glutamate. Moreover, the antinociceptive effect of DMFP in the acetic acid-induced abdominal-writhing test and the hot-plate test was not antagonized by pretreatment with a non-selective opioid receptor antagonist, naloxone. Finally, DMFP did not show any toxic effects and/or mortality in a study of acute toxicity and did not interfere with motor coordination during the Rota-rod test. Our present results show that DMFP exhibits both peripheral and central antinociceptive effects. It was suggested that its peripheral antinociceptive activity is associated with attenuated production and/or release of NO and various pro-inflammatory mediators, while central antinociceptive activity seems to be unrelated to the opioidergic system, but could involve, at least in part, an interaction with the inhibition of capsaicin-sensitive fibers and the glutamatergic system.
authors.affiliation: Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Malaysia. nurizzati@cyberauthmed.edu.my.
authors.forename: Nur Izzati
authors.initials: NI
authors.lastname: Ismail
authors.affiliation: Faculty of Pharmaceutical Sciences, UCSI University, 56000 Cheras, Malaysia. mingtatt7286@gmail.com.
authors.forename: Lee
authors.initials: L
authors.lastname: Ming-Tatt
authors.affiliation: Laboratory of Natural Products, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Malaysia. nordinlajis@gmail.com.
authors.forename: Nordin
authors.initials: N
authors.lastname: Lajis
authors.affiliation: Faculty of Industrial Sciences & Technology, University Malaysia Pahang, 26300 Gambang, Malaysia. nadeemupm@gmail.com.
authors.forename: Muhammad Nadeem
authors.initials: MN
authors.lastname: Akhtar
authors.affiliation: Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Malaysia. ahmadakira@upm.edu.my.
authors.forename: Ahmad
authors.initials: A
authors.lastname: Akira
authors.affiliation: Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Malaysia. enoch@upm.edu.my.
authors.forename: Enoch Kumar
authors.initials: EK
authors.lastname: Perimal
authors.affiliation: Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Malaysia. daud.israf@gmail.com.
authors.forename: Daud Ahmad
authors.initials: DA
authors.lastname: Israf
authors.affiliation: Department of Biomedical Sciences, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, 43400 Serdang, Malaysia. mrs@upm.edu.my.
authors.forename: Mohd Roslan
authors.initials: MR
authors.lastname: Sulaiman
mesh_terms: D000700:Analgesics / Q000008:administration & dosage* / Q000494:pharmacology; D000818:Animals; D002211:Capsaicin / Q000009:adverse effects*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D005663:Furans / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D018698:Glutamic Acid / Q000009:adverse effects*; D007274:Injections, Intraperitoneal; D007659:Ketones / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D059225:Nociception / Q000187:drug effects; D059226:Nociceptive Pain / Q000139:chemically induced / Q000188:drug therapy*
chemical_list: C000617417:3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one; D000700:Analgesics; D005663:Furans; D007659:Ketones; D018698:Glutamic Acid; D002211:Capsaicin
keywords: 3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one; TRPV1 receptor; antinociceptive activity; chalcone; glutamatergic system; opioidergic system