The effects of 5-HT1A, 5-HT1B and 5-HT1D receptor agonists on trigeminal nociceptive neurotransmission in anaesthetized rats

被引:45
作者
Cumberbatch, MJ [1 ]
Hill, RG [1 ]
Hargreaves, RJ [1 ]
机构
[1] Merck Sharp & Dohme Res Labs, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England
关键词
zolmitriptan; migraine; 5-HT1B/1D receptor; 5-HT1A receptor; CP-93,129;
D O I
10.1016/S0014-2999(98)00764-X
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Pre-clinical studies have suggested that one mechanism of antimigraine action of the 'triptan' 5-HT1B/1D receptor agonists may be through inhibition of central nociceptive transmission in the trigeminal dorsal horn. In anaesthetized rats, the 5-HT1B/1D receptor agonist, zolmitriptan (up to 3 mg kg(-1), i.v.), inhibited the action potential discharge of single trigeminal neurones to noxious electrical stimulation of the middle meningeal artery. In contrast, the selective 5-HT1B receptor agonist, CP-93,129 (3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one), and the 5-HT1B receptor selective agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) had no effect in this assay at up to 3 mg kg(-1), i.v.. Brain penetrant, triptan 5-HT1B/1D receptor agonists may therefore mediate their central trigeminal anti-nociceptive action in the rat via 5-HT1D, but not 5-HT1B or 5-HT1A, receptors. (C) 1998 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:43 / 46
页数:4
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