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兔脑皮质5-羟色胺能轴突上的自身受体和α2-肾上腺素能受体。

Autoreceptors and alpha 2-adrenoceptors at the serotonergic axons of rabbit brain cortex.

作者信息

Limberger N, Bonanno G, Späth L, Starke K

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1986 Apr;332(4):324-31. doi: 10.1007/BF00500082.

DOI:10.1007/BF00500082
PMID:2874499
Abstract

Slices of the rabbit occipito-parietal cortex were preincubated with 3H-serotonin and then superfused and stimulated electrically (2 min at 3 Hz). In the absence of drugs, the stimulation-evoked overflow of tritium was approximately 3% of the tritium content of the tissue. Unlabelled serotonin and 5-carboxamido-tryptamine, when administered in the presence of 6-nitroquipazine, reduced the evoked overflow of tritium. Their effects were antagonized by metitepin (apparent pA2 value 8.1) and (+/-)-cyanopindolol (apparent pA2 value 6.4). Metitepin, but not cyanopindolol, increased evoked tritium overflow; the effect of metitepin was greater in the presence than in the absence of nitroquipazine. The evoked overflow of tritium was also depressed by clonidine, an effect antagonized by idazoxan (apparent pA2 value 7.0) but not by prazosin. Phenylephrine caused a decrease only at high concentrations that simultaneously accelerated basal tritium efflux. Prazosin and idazoxan did not change evoked tritium overflow, and phentolamine increased it significantly only when administered in the presence of (+)-oxaprotiline. Rauwolscine produced an inhibition that was prevented by metitepin. It is concluded that the serotonergic axons of the rabbit occipitoparietal cortex possess presynaptic, release-inhibiting serotonin autoreceptors and alpha 2-adrenoceptors. The receptors appear to receive an input of endogenous serotonin and, to a lesser extent, noradrenaline, under the conditions of these in vitro experiments.

摘要

将兔枕顶叶皮质切片用³H - 5 - 羟色胺预孵育,然后进行灌流并电刺激(3Hz,持续2分钟)。在无药物存在时,刺激诱发的氚溢出量约为组织中氚含量的3%。在6 - 硝基喹哌嗪存在的情况下,给予未标记的5 - 羟色胺和5 - 羧酰胺色胺可减少诱发的氚溢出。它们的作用被甲硫平(表观pA2值为8.1)和(±) - 氰基吲哚洛尔(表观pA2值为6.4)拮抗。甲硫平而非氰基吲哚洛尔增加了诱发的氚溢出;在有硝基喹哌嗪存在时甲硫平的作用比无硝基喹哌嗪时更大。可乐定也可抑制诱发的氚溢出,其作用被咪唑克生(表观pA2值为7.0)拮抗,但不被哌唑嗪拮抗。去氧肾上腺素仅在高浓度时才引起减少,同时加速基础氚外流。哌唑嗪和咪唑克生不改变诱发的氚溢出,酚妥拉明仅在( + ) - 奥普替林存在时给药才显著增加诱发的氚溢出。萝芙木碱产生的抑制作用被甲硫平阻止。结论是兔枕顶叶皮质的5 - 羟色胺能轴突具有突触前释放抑制性5 - 羟色胺自身受体和α₂ - 肾上腺素能受体。在这些体外实验条件下,这些受体似乎接受内源性5 - 羟色胺的输入,并且在较小程度上接受去甲肾上腺素的输入。

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本文引用的文献

1
Serotonin-receptor-mediated modulation of Ca2+-dependent 5-hydroxytryptamine release from neurones of the rat brain cortex.血清素受体介导对大鼠大脑皮层神经元中钙离子依赖性5-羟色胺释放的调节。
Naunyn Schmiedebergs Arch Pharmacol. 1980 Nov;314(3):223-30. doi: 10.1007/BF00498543.
2
Comparison of the pharmacological characteristics of 5 HT1 and 5 HT2 binding sites with those of serotonin autoreceptors which modulate serotonin release.5-HT1和5-HT2结合位点的药理学特性与调节5-羟色胺释放的5-羟色胺自身受体药理学特性的比较。
Naunyn Schmiedebergs Arch Pharmacol. 1982 Dec;321(3):165-70. doi: 10.1007/BF00505480.
3
Effect of amezinium on the release and catabolism of 3H-monoamines in brain slices.
α2-肾上腺素能受体拮抗剂对5-羟色胺1A受体激动剂抑制小鼠中1-(2,5-二甲氧基-4-碘苯基)-2-氨基丙烷(DOI)诱导的头部震颤的影响。
Br J Pharmacol. 1993 Aug;109(4):1046-52. doi: 10.1111/j.1476-5381.1993.tb13727.x.
4
In vivo electrophysiological evidence for tonic activation by endogenous noradrenaline of alpha 2-adrenoceptors on 5-hydroxytryptamine terminals in the rat hippocampus.体内电生理证据表明,内源性去甲肾上腺素对大鼠海马体中5-羟色胺终端的α2-肾上腺素能受体有持续性激活作用。
Naunyn Schmiedebergs Arch Pharmacol. 1993 Mar;347(3):266-72. doi: 10.1007/BF00167444.
5
Release-inhibiting alpha 2-adrenoceptors at serotonergic axons in rat and rabbit brain cortex: evidence for pharmacological identity with alpha 2-autoreceptors.大鼠和兔大脑皮层中5-羟色胺能轴突上的释放抑制性α2-肾上腺素能受体:与α2-自身受体药理学特性相同的证据
Naunyn Schmiedebergs Arch Pharmacol. 1994 Jan;349(1):25-33. doi: 10.1007/BF00178202.
6
Inhibition of noradrenaline release via presynaptic 5-HT1B receptors of the rat vena cava.通过大鼠腔静脉的突触前5-羟色胺1B受体抑制去甲肾上腺素释放。
Naunyn Schmiedebergs Arch Pharmacol. 1987 Sep;336(3):245-50. doi: 10.1007/BF00172673.
7
Proceedings of the British Pharmacological Society. 6th-8th January, 1988. Abstracts.英国药理学会会议记录。1988年1月6日至8日。摘要
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阿米三嗪对脑片中山3H-单胺释放及分解代谢的影响。
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Du 24565, a quipazine derivative, a potent selective serotonin uptake inhibitor.Du 24565,一种喹哌嗪衍生物,一种强效选择性5-羟色胺摄取抑制剂。
Eur J Pharmacol. 1981 Mar 12;70(2):195-202. doi: 10.1016/0014-2999(81)90214-4.
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Citalopram antagonizes the stimulation by lysergic acid diethylamide of presynaptic inhibitory serotonin autoreceptors in the rat hypothalamus.西酞普兰可拮抗大鼠下丘脑中麦角酸二乙胺对突触前抑制性5-羟色胺自身受体的刺激作用。
J Pharmacol Exp Ther. 1982 Jul;222(1):220-6.
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Evidence for common pharmacological properties of [3H]5-hydroxytryptamine binding sites, presynaptic 5-hydroxytryptamine autoreceptors in CNS and inhibitory presynaptic 5-hydroxytryptamine receptors on sympathetic nerves.[3H]5-羟色胺结合位点、中枢神经系统中突触前5-羟色胺自身受体以及交感神经上抑制性突触前5-羟色胺受体的共同药理学特性的证据。
Naunyn Schmiedebergs Arch Pharmacol. 1983 Sep;324(2):116-24. doi: 10.1007/BF00497016.
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Biochem Pharmacol. 1983 Oct 15;32(20):3122-5. doi: 10.1016/0006-2952(83)90261-7.
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Stereoselective blockade at [3H]5-HT binding sites and at the 5-HT autoreceptor by propranolol.普萘洛尔对[3H]5-羟色胺结合位点及5-羟色胺自身受体的立体选择性阻断作用。
Eur J Pharmacol. 1984 Jun 1;101(3-4):289-93. doi: 10.1016/0014-2999(84)90173-0.