ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation

Olsen, Uffe Bang; Eltorp, Christina T; Ingvardsen, B K; Jørgensen, Tine Krogh; Lundbæk, Jens August; Thomsen, C.; Hansen, Anker Jón

doi:10.1016/s0014-2999(01)01556-4

Cited by 31 publications

(34 citation statements)

References 65 publications

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“…Our previous results have shown that intracerebroventricular injection of chlorpheniramine significantly decreases the number of eye wipes in the acute model of trigeminal pain [4]. It has been reported that ReN 1869 (H 1 antagonist) produces antinociception in chemical (formalin and capsaicin) but not in thermal (hot plate and tail flick) nociceptive test [1]. Moreover, it was reported that pyrilamine (H 1 antagonist) without any effect in the formalin test, produced antinociception in acetic acidinduced writhing in mice [27].…”

Section: Discussionmentioning

confidence: 99%

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The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

Khalilzadeh

Azarpey

Hazrati

2016

Asian J Pharm Clin Res

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Objective: In this study, the effect of different classes of histamine H 1 receptor antagonists (chlorpheniramine, cetirizine, and fexofenadine), µ opioid receptor agonist (morphine), and opioid receptor antagonist (naloxone) in separate and combined treatments were investigated on the acute trigeminal model of pain in rats.Methods: Eye wiping test used for induction of acute trigeminal pain by putting a drop of NaCl, 5 M solution (40 µl) on the corneal surface of the eye, and the number of eye wipes counted during the first 30 seconds.Results: Intraperitoneal injection of both chlorpheniramine and cetirizine at doses of 10 and 20 mg/kg significantly inhibited the acute trigeminal pain. However, fexofenadine did not change corneal pain response. Morphine at doses of 1.25, 2.5, and 5 mg/kg reduced eye wipe responses. Administration of both chlorpheniramine and cetirizine but not fexofenadine before morphine-enhanced morphine analgesic activity, also pretreatment of animals with naloxone inhibited morphine, chlorpheniramine, and cetirizine-induced analgesia in the acute corneal pain. Conclusion:Our results showed that chlorpheniramine as a histamine H 1 antagonist that efficiently Penetrates blood-brain barrier (BBB) and cetirizine with less penetration of BBB but not fexofenadine (an H 1 receptor antagonist with a negligible brain-accessibility) could induce analgesia in the acute corneal pain via opioidergic mechanism. Coadministration of morphine with chlorpheniramine or cetirizine could enhance its analgesic activity in the acute trigeminal model of pain in rats.

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Section: Discussionmentioning

confidence: 99%

“…For example, ReN-1869 is a novel selective H 1 receptor antagonist that has been developed for analgesic purpose [1]. It has been reported that histamine H 1 receptor knockout mice showed decreased sensitivity to nociceptive stimuli [2].…”

Section: Introductionmentioning

confidence: 99%

The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

Khalilzadeh

Azarpey

Hazrati

2016

Asian J Pharm Clin Res

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“…18) In addition, anti-histaminic drugs show antinociceptive effects on formalin-induced stimuli. [19][20][21] Thus, histamine seems to be involved in the stimulation of nociceptive fibers, and its antagonists show antinociceptive effects, considering histaminergic neurons are important for pain modulation. 22) We demonstrated that damnacanthal is the major component in the CHCl 3 -soluble phase of the Noni root.…”

Section: Discussionmentioning

confidence: 99%

The Antinociceptive and Anti-inflammatory Action of the CHCl3-Soluble Phase and Its Main Active Component, Damnacanthal, Isolated from the Root of Morinda citrifolia

Okusada

Nakamoto

Nishida

et al. 2011

Biological & Pharmaceutical Bulletin

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“…Pongamia pinnata leaves (23) and ReN1869 (15), using the same experimental edema model, which has been largely used. …”

Section: Discussionmentioning

confidence: 99%

A glycoprotein with anti-inflammatory properties secreted by an Aspergillus nidulans modified strain

Queiroz

Teixeira

Lebrun

et al. 2007

J. Venom. Anim. Toxins incl. Trop. Dis

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Total RNA from lipopolysaccharide (LPS)-stimulated rat macrophages used to treat protoplasts from an Aspergillus nidulans strain originated the RT2 regenerated strain, whose culture supernatant showed anti-inflammatory activity in Wistar rats. The protein fraction presenting such anti-inflammatory activity was purified and biochemically identified. The screening of the fraction responsible for such anti-inflammatory property was performed by evaluating the inhibition of carrageenan-induced paw edema in male Swiss mice. Biochemical analyses of the anti-inflammatory protein used chromatography, carbohydrates quantification of the protein sample, amino acids content analysis and sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). Total sugar quantification revealed 32% glycosylation of the protein fraction. Amino acid analysis of such fraction showed a peculiar pattern presenting 29% valine. SDS-PAGE revealed that the protein sample is pure and its molecular weight is about 40kDa. Intravenous injection of the isolated substance into mice significantly inhibited carrageenan-induced paw edema. The isolated glycoprotein decreased carrageenan-induced paw edema in a prostaglandin-dependent phase, suggesting an inhibitory effect of the isolated glycoprotein on prostaglandin synthesis.

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ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation

Cited by 31 publications

References 65 publications

The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

The Effect of Histamine H1 Receptor Antagonists on the Morphine-Induced Antinociception in the Acute Trigeminal Model of Nociception in Rats

The Antinociceptive and Anti-inflammatory Action of the CHCl3-Soluble Phase and Its Main Active Component, Damnacanthal, Isolated from the Root of Morinda citrifolia

A glycoprotein with anti-inflammatory properties secreted by an Aspergillus nidulans modified strain

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