Crick H, Manuel N A, Wallis D I
Department of Physiology, University of Wales, Cardiff, U.K.
Neuropharmacology. 1994 Jul;33(7):897-904. doi: 10.1016/0028-3908(94)90188-0.
The monosynaptic reflex (MSR), recorded in vitro from the neonatal rat spinal cord, was depressed by 5-hydroxytryptamine (5-HT) and 5-HT receptor agonists. The results, together with our previous findings, indicate an apparent rank order of potency: 5-carboxamidotryptamine (5-CT) > sumatriptan > methysergide > 5-HT >> 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) > 5-methoxytryptamine (5-MeOT) = 1-[3-(trifluoromethyl)phenyl]-piperazine (TFMPP) > alpha-methyl-5-hydroxytryptamine (alpha-Me 5-HT) >> (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI). The equipotent molar ratios were 5-CT 0.12, sumatriptan 0.4, methysergide 0.72, 5-HT 1.0, 8-OH-DPAT 13.3, 5-MeOT 26.7, TFMPP 31, alpha-Me 5-HT 402 and DOI > 3333. Time for peak depression from start of agonist application was 3-4 min for 5-HT, 5 min for sumatriptan and 5-MeOT, 5-7 min for alpha-Me 5-HT and 12 min for 8-OH-DPAT. The half-time for recovery from peak depression was 1.5 +/- 0.3 min for 5-HT, 2.8 +/- 0.3 min for 5-MeOT, 5.3 +/- 1.5 min for sumatriptan, 13 +/- 2.9 min for 8-OH-DPAT and > 30 min for alpha-Me 5-HT. 8-OH-DPAT induced depression of the reflex (IC50 0.85, 0.7-1.0 microM, geometric mean and 95% confidence limits) was blocked by spiperone (1 microM, apparent pA2 6.3) suggesting mediation via 5-HT1A receptors.(ABSTRACT TRUNCATED AT 250 WORDS)
从新生大鼠脊髓体外记录的单突触反射（MSR），受到5-羟色胺（5-HT）和5-HT受体激动剂的抑制。这些结果与我们之前的发现一起，表明了明显的效价顺序：5-羧酰胺色胺（5-CT）>舒马曲坦>麦角新碱>5-HT>>8-羟基-2-（二正丙基氨基）四氢萘（8-OH-DPAT）>5-甲氧基色胺（5-MeOT）=1-[3-（三氟甲基）苯基]-哌嗪（TFMPP）>α-甲基-5-羟色胺（α-Me 5-HT）>>（±）-1-（2,5-二甲氧基-4-碘苯基）-2-氨基丙烷（DOI）。等效摩尔比为5-CT 0.12、舒马曲坦0.4、麦角新碱0.72、5-HT 1.0、8-OH-DPAT 13.3、5-MeOT 26.7、TFMPP 31、α-Me 5-HT 402和DOI>3333。从开始应用激动剂到达到最大抑制的时间，5-HT为3-4分钟，舒马曲坦和5-MeOT为5分钟，α-Me 5-HT为5-7分钟，8-OH-DPAT为12分钟。从最大抑制恢复的半衰期，5-HT为1.5±0.3分钟，5-MeOT为2.8±0.3分钟，舒马曲坦为5.3±1.5分钟，8-OH-DPAT为13±2.9分钟，α-Me 5-HT大于30分钟。8-OH-DPAT诱导的反射抑制（IC50 0.85，0.7-1.0微摩尔，几何平均值和95%置信限）被螺哌隆（1微摩尔，表观pA2 6.3）阻断，提示通过5-HT1A受体介导。（摘要截断于250字）
