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1
The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies.5-羟色胺（5-HT）7型受体拮抗剂SB-269970对5-羟色胺能终末和细胞体释放5-羟色胺的影响。
Br J Pharmacol. 2001 Apr;132(7):1574-80. doi: 10.1038/sj.bjp.0703979.
2
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3
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5-HT7 receptor subtype as a mediator of the serotonergic regulation of luteinizing hormone release in the zona incerta.5-羟色胺7受体亚型作为未定带中促黄体生成素释放的5-羟色胺能调节的介质。
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Multiple 5-HT(1) autoreceptor subtypes govern serotonin release in dorsal and median raphé nuclei.多种5-羟色胺（1）自身受体亚型调控中缝背核和中缝正中核中的5-羟色胺释放。
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5-Hydroxytryptamine(1A) receptor-stimulated [(35)S]GTPgammaS binding in rat brain: absence of regional differences in coupling efficiency.5-羟色胺（1A）受体刺激大鼠脑内的[（35）S]GTPγS结合：偶联效率无区域差异。
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Evidence for presynaptic location of inhibitory 5-HT1D beta-like autoreceptors in the guinea-pig brain cortex.豚鼠大脑皮层中抑制性5-HT1Dβ样自身受体突触前定位的证据。
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Pharmacology of serotonin receptors modulating electrically-induced [3h]-norepinephrine release from isolated mammalian iris-ciliary bodies.调节从分离的哺乳动物虹膜睫状体中电诱导的[3H] - 去甲肾上腺素释放的5-羟色胺受体药理学
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SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain.SB-699551-A（3-环戊基-N-[2-(二甲基氨基)乙基]-N-[(4'-{[(2-苯乙基)氨基]甲基}-4-联苯基)甲基]丙酰胺二盐酸盐），一种新型的5-ht5A受体选择性拮抗剂，可增强5-羟色胺（5-HT）神经元功能：豚鼠脑中5-ht5A受体作为自身受体发挥作用的证据。
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5-HT7 receptor modulates GABAergic transmission in the rat dorsal raphe nucleus and controls cortical release of serotonin.5-羟色胺7受体调节大鼠中缝背核中的γ-氨基丁酸能传递并控制血清素的皮质释放。
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A 5-HT7 heteroreceptor-mediated inhibition of [3H]serotonin release in raphe nuclei slices of the rat: evidence for a serotonergic-glutamatergic interaction.5-羟色胺7型异受体介导对大鼠中缝核切片中[3H]5-羟色胺释放的抑制作用：5-羟色胺能-谷氨酸能相互作用的证据。
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Molecular cloning and tissue distribution of mRNA encoding porcine 5-HT7 receptor and its comparison with the structure of other species.猪5-羟色胺7受体编码mRNA的分子克隆、组织分布及其与其他物种结构的比较。
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本文引用的文献

1
Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist.选择性5-羟色胺（7）受体拮抗剂SB-269970-A的特性
Br J Pharmacol. 2000 Jun;130(3):539-48. doi: 10.1038/sj.bjp.0703357.
2
[(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.[（3）H]-SB-269970——一种5-羟色胺（7）受体的选择性拮抗剂放射性配体。
Br J Pharmacol. 2000 May;130(2):409-17. doi: 10.1038/sj.bjp.0703318.
3
5-CT stimulation of adenylyl cyclase activity in guinea-pig hippocampus: evidence for involvement of 5-HT7 and 5-HT1A receptors.5-CT对豚鼠海马腺苷酸环化酶活性的刺激作用：5-HT7和5-HT1A受体参与的证据
Br J Pharmacol. 1999 Sep;128(1):158-64. doi: 10.1038/sj.bjp.0702759.
4
Function and distribution of three rat 5-hydroxytryptamine7 (5-HT7) receptor isoforms produced by alternative splicing.由可变剪接产生的三种大鼠5-羟色胺7（5-HT7）受体亚型的功能与分布
Neuropharmacology. 1998 Dec;37(12):1621-32. doi: 10.1016/s0028-3908(98)00070-7.
5
SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.SB - 224289——一种新型的具有负性内在活性的选择性（人）5 - 羟色胺1B受体拮抗剂。
Br J Pharmacol. 1998 Sep;125(1):202-8. doi: 10.1038/sj.bjp.0702059.
6
Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719.人克隆5-HT7受体（长形式）的功能特性；SB-258719的拮抗剂谱
Br J Pharmacol. 1998 Jul;124(6):1300-6. doi: 10.1038/sj.bjp.0701946.
7
Differential effects of 5-HT1B/1D receptor antagonists in dorsal and median raphe innervated brain regions.5-HT1B/1D受体拮抗剂在中缝背核和中缝正中核支配的脑区中的差异效应。
Eur J Pharmacol. 1998 Apr 10;346(2-3):175-80. doi: 10.1016/s0014-2999(98)00061-2.
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Cloning, expression and pharmacology of a truncated splice variant of the human 5-HT7 receptor (h5-HT7b).人5-HT7受体（h5-HT7b）截短剪接变体的克隆、表达及药理学研究
Br J Pharmacol. 1997 Sep;122(1):126-32. doi: 10.1038/sj.bjp.0701336.
9
Four 5-hydroxytryptamine7 (5-HT7) receptor isoforms in human and rat produced by alternative splicing: species differences due to altered intron-exon organization.人类和大鼠中通过可变剪接产生的四种5-羟色胺7（5-HT7）受体亚型：内含子-外显子组织改变导致的物种差异。
J Neurochem. 1997 Apr;68(4):1372-81. doi: 10.1046/j.1471-4159.1997.68041372.x.
10
Functional characterization of the 5-HT terminal autoreceptor in the guinea-pig brain cortex.豚鼠大脑皮层中5-羟色胺终末自身受体的功能特性
Br J Pharmacol. 1996 Jan;117(2):384-8. doi: 10.1111/j.1476-5381.1996.tb15203.x.

5-羟色胺（5-HT）7型受体拮抗剂SB-269970对5-羟色胺能终末和细胞体释放5-羟色胺的影响。

The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies.

作者信息

Roberts C, Allen L, Langmead C J, Hagan J J, Middlemiss D N, Price G W

机构信息

Department of Neuroscience Research, SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW.

出版信息

Br J Pharmacol. 2001 Apr;132(7):1574-80. doi: 10.1038/sj.bjp.0703979.

DOI:10.1038/sj.bjp.0703979
PMID:11264252
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1572709/
Abstract
  1. The presence of 5-HT(7) receptor mRNA and protein in 5-HT neurons suggests that this receptor may act as a 5-HT autoreceptor. In this study, the effect of the 5-HT(7) receptor antagonist, SB-269970 ((R)-1-[3-hydroxy phenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine), was investigated on 5-HT release in the guinea-pig and rat cortex and the rat dorsal raphe nucleus (DRN), using the techniques of in vitro [(3)H]-5-HT release or fast cyclic voltammetry, respectively. 2. Cortical slices were loaded with [(3)H]-5-HT and release was evoked by electrical stimulation. 5-CT inhibited the evoked release of [(3)H]-5-HT in a concentration-dependent manner. SB-269970 had no significant effect on [(3)H]-5-HT release while the 5-HT(1B) receptor antagonist, SB-224289 significantly potentiated [(3)H]-5-HT release. In addition, SB-269970 was unable to attenuate the 5-CT-induced inhibition of release while SB-224289 produced a rightward shift of the 5-CT response, generating estimated pK(B) values of 7.8 and 7.6 at the guinea-pig and rat terminal 5-HT autoreceptors respectively. 3. Rat DRN slices were electrically stimulated and the evoked 5-HT efflux detected by voltammetric analysis. 8-OH-DPAT inhibited evoked 5-HT efflux and was fully reversed by WAY 100635. SB-269970 had no effect on either 5-HT efflux per se or 8-OH-DPAT-induced inhibition of 5-HT efflux. In addition, 5-CT inhibited 5-HT efflux in a concentration-dependent manner. SB-269970 was unable to attenuate the 5-CT-induced inhibition of 5-HT efflux. 4. In conclusion, we were unable to provide evidence to suggest a 5-HT autoreceptor role for 5-HT(7) receptors. However, investigations with more selective 5-HT(7) receptor agonists are needed to confirm the data reported here.
摘要
  1. 5-羟色胺（5-HT）神经元中5-HT(7)受体信使核糖核酸（mRNA）和蛋白的存在表明，该受体可能作为一种5-HT自身受体发挥作用。在本研究中，使用体外[³H]-5-HT释放技术或快速循环伏安法，分别研究了5-HT(7)受体拮抗剂SB-269970（(R)-1-[3-羟基苯基）磺酰基]-2-[2-(4-甲基-1-哌啶基)乙基]吡咯烷）对豚鼠和大鼠皮层以及大鼠中缝背核（DRN）中5-HT释放的影响。2. 皮层切片用[³H]-5-HT加载，通过电刺激诱发释放。5-羧色胺（5-CT）以浓度依赖性方式抑制[³H]-5-HT的诱发释放。SB-269970对[³H]-5-HT释放无显著影响，而5-HT(1B)受体拮抗剂SB-224289显著增强[³H]-5-HT释放。此外，SB-269970无法减弱5-CT诱导的释放抑制，而SB-224289使5-CT反应向右移位，在豚鼠和大鼠终末5-HT自身受体处产生的估计解离常数（pK(B)）值分别为7.8和7.6。3. 对大鼠DRN切片进行电刺激，并通过伏安分析检测诱发的5-HT流出。8-羟基二丙胺基四氢萘（8-OH-DPAT）抑制诱发的5-HT流出，并被WAY 100635完全逆转。SB-269970对5-HT流出本身或8-OH-DPAT诱导的5-HT流出抑制均无影响。此外，5-CT以浓度依赖性方式抑制5-HT流出。SB-269970无法减弱5-CT诱导的5-HT流出抑制。4. 总之,我们无法提供证据表明5-HT(7)受体具有5-HT自身受体作用。然而，需要用更具选择性的5-HT(7)受体激动剂进行研究以证实此处报道的数据。