Investigation Into the Role of Histamine Receptors in Rodent Antinociception

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• 作者：Lamberti ; Claudia ; Bartolini ; Alessandro ; Ghelardini ; Carla ; Malmberg-Aiello ; Petra
• 关键词：Analgesia ; Antinociception ; Pain ; Burimamide ; Impromidine ; (R)-α ; -methylhistamine ; Histamine H₂-receptor agonist ; Histamine H₂-receptor antagonist ; Histamine H₃-receptor antagonist ; Histamine H₁-receptor ant
• 刊名：Pharmacology Biochemistry and Behavior
• 出版年：1996
• 出版时间：March, 1996
• 年：1996
• 卷：53
• 期：3
• 页码：567-574
• 全文大小：772 K

文摘

The aim of the present study is to elucidate the confusion that exists in the literature concerning which receptor subtype is involved in mediating histamine antinociception. To this purpose impromidine 3HCl and burimamide were used. Because both substances have been described to block histamine H₃-receptor, and, at higher doses, also to act on the postsynaptic site as agonist and antagonist, respectively, they were administered in a wide range of ICV doses, to distinguish the effects due to action on different receptors. Experiments were performed in mice and rats by means of tests inducing three different kinds of noxious stimuli: mechanical (paw pressure), chemical (abdominal constriction), and thermal (hot plate). Both substances showed, at the lowest doses tested, antinociception, which was antagonized by the selective H₃-receptor agonist, (R)-α-methylhistamine 2HCl (RAMH) (10 mg/kg SC in mice or 0.5 μg per rat ICV). At higher doses impromidine was antinociceptive while burimamide was hypernociceptive, in accordance with their opposite action on the H₂-receptor. It is suggested that the histaminergic system modulates nociception via activation of the H₂-receptor.