Albeit conflicting, evidence suggests that 5-HT3 receptor partial agonists as well as alpha2NON-A-adrenoceptor agonists might be involved in antinociception. MD-354 (m-chlorophenylguanidine) can be viewed as the first example of a rather selective 5-HT3/alpha2B-adrenergic ligand. In a tail-flick test in mice, subcutaneous administration of MD-354 doses up to 30 mg/kg did not produce antinociception and failed to antagonize the effect of clonidine (ED50=0.5 mg/kg), but a combination of an inactive de of clonidine (0.25 mg/kg) that produced only 13% maximal possible effect (MPE) with an inactive dose of MD-354 (10 mg/kg, MPE=8%) produced an antinociceptive effect (MPE=83%). In the hot-plate assay, neither subcutaneous administration of MD-354 (3 to 30 mg/kg) alone nor in combination with clonidine (ED50=0.8 mg/kg) produced an antinociceptive effect. MD-354 was demonstrated to potentiate the antinociceptive effect of clonidine in the tail-flick assay, but its underlying mechanism remains to be determined.

译文

尽管相互矛盾,但证据表明5-HT3受体部分激动剂以及alpha2NON-A-adrenoceptor激动剂可能参与了抗伤害感受。MD-354 (间氯苯基胍) 可以被视为相当选择性的5-HT3/alpha2B-adrenergic配体的第一个例子。在小鼠的甩尾试验中,皮下施用高达30 mg/kg的MD-354剂量不会产生抗伤害感受,也不能拮抗可乐定的作用 (ED50 = 0.5 mg/kg),但是,仅产生13% 最大可能效应 (MPE) 的非活性可乐定de (0.25 mg/kg) 与非活性剂量的MD-354 (10 mg/kg,MPE = 8%) 的组合产生抗伤害感受效应 (MPE = 83%)。在热板测定中,单独皮下施用MD-354 (3至30 mg/kg) 或与可乐定 (ED50 = 0.8 mg/kg) 组合均不产生抗伤害感受作用。在甩尾试验中,已证明MD-354增强可乐定的抗伤害感受作用,但其潜在机制仍有待确定。

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