Excitatory and inhibitory 5-hydroxytryptamine (5-HT) receptors expressed in the isolated porcine uterine muscles.
Excitatory and inhibitory 5-hydroxytryptamine (5-HT) receptors expressed in the isolated porcine uterine muscles.
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离体猪子宫肌肉中表达的兴奋性和抑制性 5-羟色胺 (5-HT) 受体。
DOI：
10.1016/j.ejphar.2008.10.019
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发表时间：
2008
影响因子：
5
通讯作者：
T. Taneike
中科院分区：
文献类型：
--
作者：
Tatsuro Nakamura;T. Kitazawa;Jinshan Cao;T. Iwamoto;H. Teraoka;K. Kadota;T. Taneike
5-羟色胺 (5-HT) 受体介导 5-HT 对非妊娠猪子宫带收缩性的兴奋和抑制作用。通过分子生物学研究检测5-HT2A和5-HT7受体的表达。免疫组织化学观察含5-HT的细胞。在自发收缩的子宫环肌层中，5-HT 引起收缩活动的抑制。 SB269970（5-HT7 受体拮抗剂，10 nM）将 5-HT 的浓度-抑制曲线向右移动，但较高浓度的 SB269970 (100 nM–1 μM) 将单相曲线更改为双相曲线（对 5-HT 的兴奋性和抑制性反应的混合）。添加酮色林（5-HT2 受体拮抗剂，10 nM–1 μM）可降低 5-HT 的兴奋作用。 5-HT 在抑制纵向肌自发收缩方面效果较差。 Ketanserin 增强了抑制反应，SB269970 将抑制反应逆转为兴奋反应。在 SB269970 存在的情况下，α-甲基-5-HT 在增加纵向肌肉收缩性方面与 5-HT 等效，酮色林竞争性抑制对 α-甲基-5-HT 的反应 (pKd=8.78)。 RT-PCR 和实时 PCR 证明了猪子宫肌层中 5-HT2A 受体和 5-HT7 受体 mRNA 的肌层依赖性表达。仅在子宫腺细胞中检测到 5-HT 免疫反应性，这些细胞位于子宫环肌层附近。在具有子宫内膜的纵向和环形肌层中，化合物48/80和酮舍林不改变自发收缩力，但SB269970显着增加环形肌的收缩活性。总之，非妊娠猪的子宫中存在兴奋性5-HT2A和抑制性5-HT7。含有内源性5-HT的细胞主要存在于猪的子宫腺中。讨论了 5-HT 及其受体在调节猪子宫自发收缩力中的可能作用。
5-Hydroxytryptamine (5-HT) receptors mediating excitatory and inhibitory actions of 5-HT on contractility of uterine strips from non-pregnant pigs were characterized. Expression of 5-HT2Aand 5-HT7receptors was examined by molecular biological study. 5-HT-containing cells were observed immunohistochemically. In the spontaneously contracting uterine circular muscle layers, 5-HT caused inhibition of contractile activity. SB269970 (5-HT7receptor antagonist, 10 nM) shifted the concentration-inhibition curve of 5-HT to the right, but higher concentrations of SB269970 (100 nM–1 μM) changed the monophasic curve to a biphasic curve (mixture of excitatory and inhibitory responses to 5-HT). Addition of ketanserin (5-HT2receptor antagonist, 10 nM–1 μM) decreased the excitatory effects of 5-HT. 5-HT was less effective in inhibiting the spontaneous contraction in the longitudinal muscles. Ketanserin enhanced the inhibitory responses and SB269970 reversed the inhibitory responses to excitatory responses. In the presence of SB269970, α-methyl-5-HT was equipotent to 5-HT in increasing contractility of longitudinal muscle and ketanserin competitively inhibited the responses to α-methyl-5-HT (pKd=8.78). Muscle layer-dependent expression of both 5-HT2Areceptor and 5-HT7receptor mRNAs in the porcine uterine muscle layers was demonstrated by RT-PCR and real-time PCR. 5-HT immunoreactivity was detected only in uterine gland cells, which were localized near the uterine circular muscle layers. In the longitudinal and circular muscle layers with endometrium, compounds 48/80 and ketanserin did not change the spontaneous contractility, but SB269970 significantly increased the contractile activity of the circular muscle. In conclusion, excitatory 5-HT2Aand inhibitory 5-HT7are present in the uterus of non-pregnant pigs. Endogenous 5-HT containing cells are mainly present in uterine glands of the pig. The possible roles of 5-HT and its receptors in regulation of porcine uterine spontaneous contractility are discussed.