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5-HT2A 受体在 C57BL/6N 小鼠中的药理学和行为特征。

Pharmacological and behavioral characterization of the 5-HT2A receptor in C57BL/6N mice.

机构信息

Drexel University College of Medicine, Philadelphia, PA 19102, USA.

出版信息

Psychopharmacology (Berl). 2011 Jun;215(3):581-93. doi: 10.1007/s00213-011-2207-6. Epub 2011 Feb 22.

DOI:10.1007/s00213-011-2207-6
PMID:21340474
Abstract

RATIONALE

The serotonin (5-HT) 2A receptor is implicated in numerous psychiatric disorders, making it an important, clinically relevant target. Despite the availability of transgenic mouse lines, the native mouse 5-HT(2A) receptor is not well-characterized.

OBJECTIVES

The goals of the current study were to determine 5-HT(2A) and 5-HT(2C) receptor densities in mouse cortex, establish a pharmacological profile of the mouse 5-HT(2A) receptor, and determine the effects of chronic drug treatment on 5-HT(2A) receptor density and 5-HT(2A) receptor-mediated behavior.

METHODS

Receptor densities were determined in cortex and frontal cortex via saturation binding assays using [(3)H]ketanserin or [(3)H]mesulergine. A pharmacological profile was established by displacing [(3)H]ketanserin binding with several ligands. Chronic treatment with 5-HT(2A/2C) receptor agonist, 2,5-dimethoxy-4-iodoamphetamine (DOI), 5-HT(2A) receptor antagonist, MDL 11939, or vehicle was followed by 5-HT(2A) receptor density determination. Head twitch responses (HTRs) were counted on select days.

RESULTS

Mice had high 5-HT(2A), but low 5-HT(2C) receptor densities. Ligand binding affinities for mouse 5-HT(2A) receptors correlated with rat, but not rabbit or human, affinities. Chronically DOI-treated mice displayed reduced HTRs and 5-HT(2A) receptor density compared to saline-treated mice. Receptor density was unchanged following chronic treatment with MDL 11939.

CONCLUSIONS

The current study provides some basic information about mouse 5-HT(2A) and 5-HT(2C) receptors and provides comparisons to rats, rabbits, and humans. The current chronic agonist treatment study demonstrated an important similarity between the 5-HT(2A) receptor in mice, rats, and rabbits, while antagonist treatment revealed an interesting difference from previous studies in rabbits.

摘要

背景

血清素（5-HT）2A 受体与许多精神疾病有关，是一个重要的、与临床相关的靶点。尽管有转基因小鼠品系，但内源性小鼠 5-HT(2A)受体尚未得到很好的描述。

目的

本研究的目的是确定小鼠皮质中 5-HT(2A)和 5-HT(2C)受体的密度，建立小鼠 5-HT(2A)受体的药理学特征，并确定慢性药物治疗对 5-HT(2A)受体密度和 5-HT(2A)受体介导的行为的影响。

方法

通过使用 [(3)H]酮色林或 [(3)H]mesulergine进行饱和结合测定，在皮质和额皮质中确定受体密度。通过用几种配体置换 [(3)H]酮色林结合来建立药理学特征。用 5-HT(2A/2C)受体激动剂 2,5-二甲氧基-4-碘苯丙胺（DOI）、5-HT(2A)受体拮抗剂 MDL 11939 或载体进行慢性治疗，然后测定 5-HT(2A)受体密度。选择性天数计数头部抽搐反应（HTRs）。

结果

小鼠具有高 5-HT(2A)，但低 5-HT(2C)受体密度。小鼠 5-HT(2A)受体的配体结合亲和力与大鼠相关，但与兔或人无关。与盐水处理的小鼠相比，慢性 DOI 处理的小鼠显示出减少的 HTRs 和 5-HT(2A)受体密度。用 MDL 11939 进行慢性治疗后，受体密度没有变化。

结论

本研究提供了一些关于小鼠 5-HT(2A)和 5-HT(2C)受体的基本信息，并与大鼠、兔和人进行了比较。目前的慢性激动剂治疗研究表明，小鼠、大鼠和兔的 5-HT(2A)受体之间存在重要的相似性，而拮抗剂治疗则揭示了与之前在兔中进行的研究的有趣差异。

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