Bardin L, Tarayre J P, Koek W, Colpaert F C
Centre de Recherche Pierre-Fabre, 17 Avenue Jean Moulin, F-81106 Cédex, Castres, France.
Eur J Pharmacol. 2001 Jun 8;421(2):109-14. doi: 10.1016/s0014-2999(01)01029-9.
The experiments examined antinociceptive and intrinsic behavioral effects induced by the prototypical 5-HT1A receptor agonist 8-OH-DPAT (8-hydroxy-2-[di-n-propylamino] tetralin) in rats. 8-OH-DPAT (0.01-2.5 mg/kg, subcutaneous (s.c.)) reduced both the paw licking and paw elevation induced by (2.5%) formalin injection into the plantar surface of the right hindpaw; it also produced forepaw treading. All of these effects were completely blocked by pretreatment with WAY 100635 (N-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride) (0.16 mg/kg, s.c.); prazosin (0.63 mg/kg, s.c.) inhibited forepaw treading, but not 8-OH-DPAT's action on paw elevation and paw licking. Repeated injection of 8-OH-DPAT (0.63 mg/kg, s.c.) twice daily for 4 days, markedly reduced 8-OH-DPAT's ability to produce forepaw treading, but exerted only little and inconsistent effects on its paw licking and paw elevation-inhibiting action. The data indicate that 8-OH-DPAT exerts an analgesic action in the formalin model of tonic nociceptive pain; this action is mediated by 5-HT(1A) receptors, and is not confounded by the productive sign (i.e., forepaw treading) of the 5-HT syndrome which 8-OH-DPAT also induces.
这些实验研究了典型的5-羟色胺1A受体激动剂8-OH-DPAT（8-羟基-2-[二正丙基氨基]四氢萘）对大鼠的抗伤害感受和内在行为影响。8-OH-DPAT（0.01 - 2.5毫克/千克，皮下注射）减少了右后足底注射（2.5%）福尔马林所诱导的舔爪和抬爪行为；它还引发了前爪踩踏。所有这些效应都被预先注射WAY 100635（N-(2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基)-N-(2-吡啶基)环己烷甲酰胺三盐酸盐）（0.16毫克/千克，皮下注射）完全阻断；哌唑嗪（0.63毫克/千克，皮下注射）抑制了前爪踩踏，但不影响8-OH-DPAT对抬爪和舔爪的作用。每天两次重复注射8-OH-DPAT（0.63毫克/千克，皮下注射），持续4天，显著降低了8-OH-DPAT引发前爪踩踏的能力，但对其舔爪和抑制抬爪的作用仅有微小且不一致的影响。数据表明，8-OH-DPAT在福尔马林诱发的持续性伤害性疼痛模型中发挥镇痛作用；该作用由5-羟色胺(1A)受体介导，且不受8-OH-DPAT所诱导的5-羟色胺综合征的阳性体征（即前爪踩踏）的干扰。
