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1
CP-93,129, a potent and selective 5-HT1B receptor agonist blocks neurogenic plasma extravasation within rat but not guinea-pig dura mater.CP-93,129，一种强效且具选择性的5-羟色胺1B受体激动剂，可阻断大鼠硬脑膜内的神经源性血浆外渗，但对豚鼠硬脑膜无效。
Br J Pharmacol. 1991 Sep;104(1):3-4. doi: 10.1111/j.1476-5381.1991.tb12374.x.
2
Time-dependent blockade of neurogenic plasma extravasation in dura mater by 5-HT1B/D agonists and endopeptidase 24.11.5-HT1B/D激动剂和内肽酶24.11对硬脑膜中神经源性血浆外渗的时间依赖性阻断作用
Br J Pharmacol. 1993 Feb;108(2):331-5. doi: 10.1111/j.1476-5381.1993.tb12805.x.
3
Further characterization of the putative 5-HT receptor which mediates blockade of neurogenic plasma extravasation in rat dura mater.对介导大鼠硬脑膜神经源性血浆外渗阻断作用的假定5-羟色胺受体的进一步表征。
Br J Pharmacol. 1991 Jun;103(2):1421-8. doi: 10.1111/j.1476-5381.1991.tb09805.x.
4
The antimigraine drug, sumatriptan (GR43175), selectively blocks neurogenic plasma extravasation from blood vessels in dura mater.抗偏头痛药物舒马曲坦（GR43175）可选择性地阻断硬脑膜血管的神经源性血浆外渗。
Br J Pharmacol. 1990 Jan;99(1):202-6. doi: 10.1111/j.1476-5381.1990.tb14679.x.
5
The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater.5-羟色胺1D受体拮抗剂GR-127,935可阻止舒马曲坦对豚鼠硬脑膜内神经源性血浆外渗的抑制作用，但不能阻止CP-122,288和5-羧色胺的抑制作用。
Neuropharmacology. 1997 Jan;36(1):83-91. doi: 10.1016/s0028-3908(96)00149-9.
6
Evidence for 5-HT1B/1D receptors mediating the antimigraine effect of sumatriptan and dihydroergotamine.5-羟色胺1B/1D受体介导舒马曲坦和双氢麦角胺抗偏头痛作用的证据。
Cephalalgia. 1991 Sep;11(4):165-8. doi: 10.1046/j.1468-2982.1991.1104165.x.
7
5-Carboxamido-tryptamine, CP-122,288 and dihydroergotamine but not sumatriptan, CP-93,129, and serotonin-5-O-carboxymethyl-glycyl -tyrosinamide block dural plasma protein extravasation in knockout mice that lack 5-hydroxytryptamine1B receptors.5-羧酰胺基色胺、CP-122,288和双氢麦角胺可阻断缺乏5-羟色胺1B受体的基因敲除小鼠的硬脑膜血浆蛋白外渗，但舒马曲坦、CP-93,129和5-羟色胺-5-O-羧甲基-甘氨酰-酪氨酰胺则不能。
Mol Pharmacol. 1996 May;49(5):761-5.
8
Effects of PNU-109,291, a selective 5-HT1D receptor agonist, on electrically induced dural plasma extravasation and capsaicin-evoked c-fos immunoreactivity within trigeminal nucleus caudalis.选择性5-HT1D受体激动剂PNU-109,291对电诱导的硬脑膜血浆外渗及三叉神经尾侧核内辣椒素诱发的c-fos免疫反应性的影响。
Neuropharmacology. 1999 Jul;38(7):1043-53. doi: 10.1016/s0028-3908(99)00032-5.
9
The in vivo pharmacological profile of a 5-HT1 receptor agonist, CP-122,288, a selective inhibitor of neurogenic inflammation.5-羟色胺1（5-HT1）受体激动剂CP-122,288（一种神经源性炎症的选择性抑制剂）的体内药理学特征。
Br J Pharmacol. 1995 Nov;116(5):2385-90. doi: 10.1111/j.1476-5381.1995.tb15084.x.
10
Role of endothelin in mediating neurogenic plasma extravasation in rat dura mater.内皮素在介导大鼠硬脑膜神经源性血浆外渗中的作用。
Pain. 1996 Feb;64(2):315-322. doi: 10.1016/0304-3959(95)00106-9.

引用本文的文献

1
Presynaptic 5-HT(1B) receptor-mediated serotonergic inhibition of glutamate transmission in the bed nucleus of the stria terminalis.终纹床核中 5-羟色胺能神经元突触前 5-HT（1B）受体对谷氨酸传递的抑制作用。
Neuroscience. 2010 Feb 17;165(4):1390-401. doi: 10.1016/j.neuroscience.2009.11.071. Epub 2009 Dec 3.
2
Migraine: where and how does the pain originate?偏头痛：疼痛源自何处以及如何产生？
Exp Brain Res. 2009 Jun;196(1):179-93. doi: 10.1007/s00221-009-1756-y. Epub 2009 Mar 14.
3
Time-dependent blockade of neurogenic plasma extravasation in dura mater by 5-HT1B/D agonists and endopeptidase 24.11.5-HT1B/D激动剂和内肽酶24.11对硬脑膜中神经源性血浆外渗的时间依赖性阻断作用
Br J Pharmacol. 1993 Feb;108(2):331-5. doi: 10.1111/j.1476-5381.1993.tb12805.x.
4
Selective 5-HT1D alpha serotonin receptor gene expression in trigeminal ganglia: implications for antimigraine drug development.三叉神经节中5-羟色胺1Dα选择性血清素受体基因表达：对抗偏头痛药物研发的启示
Proc Natl Acad Sci U S A. 1994 Apr 26;91(9):3666-9. doi: 10.1073/pnas.91.9.3666.
5
Blockade by oral or parenteral RPR 100893 (a non-peptide NK1 receptor antagonist) of neurogenic plasma protein extravasation within guinea-pig dura mater and conjunctiva.口服或肠胃外给予RPR 100893（一种非肽类NK1受体拮抗剂）对豚鼠硬脑膜和结膜内神经源性血浆蛋白外渗的阻断作用。
Br J Pharmacol. 1994 Jul;112(3):920-4. doi: 10.1111/j.1476-5381.1994.tb13168.x.
6
Effect of a 5-HT1 receptor agonist, CP-122,288, on oedema formation induced by stimulation of the rat saphenous nerve.5-羟色胺1（5-HT1）受体激动剂CP-122,288对刺激大鼠隐神经诱导的水肿形成的影响。
Br J Pharmacol. 1995 May;115(1):1-2. doi: 10.1111/j.1476-5381.1995.tb16310.x.
7
Inhibition of excitatory non-adrenergic non-cholinergic bronchoconstriction in guinea-pig airways in vitro by activation of an atypical 5-HT receptor.通过激活一种非典型5-羟色胺受体对豚鼠气道体外兴奋性非肾上腺素能非胆碱能支气管收缩的抑制作用
Br J Pharmacol. 1994 Apr;111(4):1095-102. doi: 10.1111/j.1476-5381.1994.tb14857.x.
8
CP-93,129, sumatriptan, dihydroergotamine block c-fos expression within rat trigeminal nucleus caudalis caused by chemical stimulation of the meninges.CP-93,129、舒马曲坦、双氢麦角胺可阻断由化学刺激脑膜引起的大鼠三叉神经尾侧核内c-fos的表达。
Br J Pharmacol. 1992 Jun;106(2):409-15. doi: 10.1111/j.1476-5381.1992.tb14348.x.

本文引用的文献

1
Neurogenically mediated leakage of plasma protein occurs from blood vessels in dura mater but not brain.神经源性介导的血浆蛋白渗漏发生于硬脑膜血管而非脑内血管。
J Neurosci. 1987 Dec;7(12):4129-36. doi: 10.1523/JNEUROSCI.07-12-04129.1987.
2
Ergot alkaloids block neurogenic extravasation in dura mater: proposed action in vascular headaches.麦角生物碱可阻断硬脑膜的神经源性血管外渗：对血管性头痛的作用机制探讨
Ann Neurol. 1988 Dec;24(6):732-7. doi: 10.1002/ana.410240607.
3
Species differences in the pharmacology of terminal 5-HT autoreceptors in mammalian brain.哺乳动物脑中5-羟色胺（5-HT）终末自身受体药理学的种属差异。
Trends Pharmacol Sci. 1989 Apr;10(4):130-2. doi: 10.1016/0165-6147(89)90159-4.
4
3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.3-(1,2,5,6-四氢吡啶-4-基)吡咯并[3,2-b]吡啶-5-酮：一种强效且选择性的血清素（5-HT1B）激动剂，是5-甲氧基-3-(1,2,5,6-四氢吡啶-4-基)吲哚的旋转受限酚类类似物。
J Med Chem. 1990 Aug;33(8):2087-93. doi: 10.1021/jm00170a007.
5
The antimigraine drug, sumatriptan (GR43175), selectively blocks neurogenic plasma extravasation from blood vessels in dura mater.抗偏头痛药物舒马曲坦（GR43175）可选择性地阻断硬脑膜血管的神经源性血浆外渗。
Br J Pharmacol. 1990 Jan;99(1):202-6. doi: 10.1111/j.1476-5381.1990.tb14679.x.

CP-93,129，一种强效且具选择性的5-羟色胺1B受体激动剂，可阻断大鼠硬脑膜内的神经源性血浆外渗，但对豚鼠硬脑膜无效。

CP-93,129, a potent and selective 5-HT1B receptor agonist blocks neurogenic plasma extravasation within rat but not guinea-pig dura mater.

作者信息

Matsubara T, Moskowitz M A, Byun B

机构信息

Stroke Research Laboratory, Massachusetts General Hospital, Harvard Medical School, Boston 02114.

出版信息

Br J Pharmacol. 1991 Sep;104(1):3-4. doi: 10.1111/j.1476-5381.1991.tb12374.x.

DOI:10.1111/j.1476-5381.1991.tb12374.x
PMID:1664765
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1908303/
Abstract

Pretreatment with CP-93,129 blocked plasma extravasation in rat dura mater induced by electrical trigeminal ganglion stimulation when administered at greater than or equal to 140 nmol kg-1, i.v. but did not affect plasma leakage in guinea-pig at 460 or 1400 nmol kg-1. Sumatriptan, a 5-HT1D-like receptor agonist, blocked plasma extravasation in the guinea-pig model when administered at 7 nmol kg-1. In as much as CP-93,129 binds with micromolar affinities to 5-HT1A, 5-HT1C, 5-HT1D, and 5-HT2 recognition sites, and with nanomolar affinity to the 5-HT1B receptor subtype, blockade of plasma extravasation in the rat dura mater may be mediated by 5-HT1B receptors whereas the 5-HT1D receptor may be more relevant to the guinea-pig.

摘要

当静脉注射剂量大于或等于140 nmol/kg时，CP - 93,129预处理可阻断电刺激三叉神经节诱导的大鼠硬脑膜血浆外渗，但在460或1400 nmol/kg时对豚鼠的血浆渗漏没有影响。舒马曲坦是一种5 - HT1D样受体激动剂，当以7 nmol/kg给药时，可阻断豚鼠模型中的血浆外渗。由于CP - 93,129以微摩尔亲和力与5 - HT1A、5 - HT1C、5 - HT1D和5 - HT2识别位点结合，并以纳摩尔亲和力与5 - HT1B受体亚型结合，大鼠硬脑膜中血浆外渗的阻断可能由5 - HT1B受体介导，而5 - HT1D受体可能与豚鼠的关系更密切。