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本文引用的文献

1
PPADS selectively antagonizes P2X-purinoceptor-mediated responses in the rabbit urinary bladder.PPADS可选择性拮抗兔膀胱中P2X嘌呤受体介导的反应。
Br J Pharmacol. 1993 Dec;110(4):1491-5. doi: 10.1111/j.1476-5381.1993.tb13990.x.
2
The use of the slowly degradable analog, alpha, beta-methylene ATP, to produce desensitisation of the P2-purinoceptor: effect on non-adrenergic, non-cholinergic responses of the guinea-pig urinary bladder.使用缓慢降解类似物α,β-亚甲基ATP诱导P2嘌呤受体脱敏：对豚鼠膀胱非肾上腺素能、非胆碱能反应的影响
Eur J Pharmacol. 1982 Dec 24;86(2):291-4. doi: 10.1016/0014-2999(82)90330-2.
3
Purinergic receptors: photoaffinity analog of adenosine triphosphate is a specific adenosine triphosphate antagonist.嘌呤能受体：三磷酸腺苷的光亲和类似物是一种特异性三磷酸腺苷拮抗剂。
Science. 1980 Jun 13;208(4449):1273-6. doi: 10.1126/science.6103581.
4
A direct method for recording tension changes in the wall of small blood vessels in vitro.一种体外记录小血管壁张力变化的直接方法。
Agents Actions. 1972;2(5):257-60. doi: 10.1007/BF02087051.
5
Purine-mediated relaxation and constriction of isolated rabbit mesenteric artery are not endothelium-dependent.嘌呤介导的离体兔肠系膜动脉舒张和收缩不依赖于内皮。
Eur J Pharmacol. 1985 Dec 3;118(3):221-9. doi: 10.1016/0014-2999(85)90132-3.
6
P2-purinoceptors of two subtypes in the rabbit mesenteric artery: reactive blue 2 selectively inhibits responses mediated via the P2y-but not the P2x-purinoceptor.兔肠系膜动脉中两种亚型的P2嘌呤受体：活性蓝2选择性抑制通过P2Y嘌呤受体而非P2X嘌呤受体介导的反应。
Br J Pharmacol. 1987 Feb;90(2):383-91. doi: 10.1111/j.1476-5381.1987.tb08968.x.
7
A pharmacological study of the rabbit saphenous artery in vitro: a vessel with a large purinergic contractile response to sympathetic nerve stimulation.兔隐动脉的体外药理学研究：一种对交感神经刺激有大量嘌呤能收缩反应的血管。
Br J Pharmacol. 1987 Jan;90(1):111-20. doi: 10.1111/j.1476-5381.1987.tb16830.x.
8
The contributions of noradrenaline and ATP to the responses of the rabbit central ear artery to sympathetic nerve stimulation depend on the parameters of stimulation.去甲肾上腺素和三磷酸腺苷对兔中耳动脉交感神经刺激反应的贡献取决于刺激参数。
Eur J Pharmacol. 1986 Apr 2;122(3):291-300. doi: 10.1016/0014-2999(86)90409-7.
9
Effects of reserpine and 6-hydroxydopamine on the adrenergic and purinergic components of sympathetic nerve responses of the rabbit saphenous artery.利血平和6-羟基多巴胺对兔隐动脉交感神经反应中肾上腺素能和嘌呤能成分的影响。
Br J Pharmacol. 1987 Dec;92(4):871-80. doi: 10.1111/j.1476-5381.1987.tb11393.x.
10
Is there a basis for distinguishing two types of P2-purinoceptor?是否有依据区分两种类型的P2嘌呤受体？
Gen Pharmacol. 1985;16(5):433-40. doi: 10.1016/0306-3623(85)90001-1.

PPADS对兔离体血管中P2X嘌呤受体的选择性拮抗作用。

Selective antagonism by PPADS at P2X-purinoceptors in rabbit isolated blood vessels.

作者信息

Ziganshin A U, Hoyle C H, Lambrecht G, Mutschler E, Bümert H G, Burnstock G

机构信息

Department of Anatomy and Developmental Biology, University College London.

出版信息

Br J Pharmacol. 1994 Mar;111(3):923-9. doi: 10.1111/j.1476-5381.1994.tb14827.x.

DOI:10.1111/j.1476-5381.1994.tb14827.x
PMID:8019770
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1910106/
Abstract
  1. Pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS), a P2-purinoceptor antagonist, was investigated for its ability to antagonize: (1) P2X-purinoceptor-mediated contractions of the rabbit central ear artery and saphenous artery evoked by either alpha,beta-methylene ATP (alpha,beta-MeATP) or electrical field stimulation (EFS); (2) P2Y-purinoceptor-mediated relaxations of the rabbit mesenteric artery; (3) endothelium-dependent and endothelium-independent, P2Y-purinoceptor-mediated relaxations of the rabbit aorta. 2. alpha,beta-MeATP (0.1-100 microM) caused concentration-dependent contractions of the rabbit ear and saphenous arteries. The negative log[alpha,beta-MeATP] that produced a contraction equivalent to the EC25 for noradrenaline (ear artery) or histamine (saphenous artery) in the absence of PPADS was 6.60 +/- 0.18 (9) and 6.18 +/- 0.17 (9) in the ear artery and saphenous artery, respectively. These effects of exogenous alpha,beta-MeATP were concentration-dependently inhibited by PPADS (1-30 microM). In the ear artery, the negative log[alpha,beta-MeATP] producing a contractile response equivalent to the EC25 of noradrenaline, in the presence of PPADS at 1, 3 and 10 microM was 6.16 +/- 0.18 (8), 5.90 +/- 0.18 (8) and 4.72 +/- 0.36 (8), respectively (P < 0.01). In the saphenous artery, the negative log[alpha,beta-MeATP] values equivalent to the EC25 for histamine in the presence of PPADS at concentrations of 1, 3, 10 and 30 microM were 5.90 +/- 0.19 (8), 5.73 +/- 0.16 (8), 4.99 +/- 0.14 (8) and 4.51 +/- 0.13 (8), respectively (P < 0.01). 3. PPADS at a concentration of 1 microM had no effect on contractions of the ear artery evoked by EFS (4-64 Hz; 1 microM phentolamine present). At higher concentrations (3-30 MicroM) it caused concentration dependent inhibition of neurogenic contractions. In the saphenous artery, PPADS (1-30 MicroM) concentration-dependently inhibited contractions evoked by EFS at frequencies of 4, 8 and 16 Hz. Contractions evoked by EFS at frequencies of 32 and 64 Hz were significantly inhibited by PPADS only at concentrations of 10 and 30 MicroM.4. PPADS (30 MicroM) had no effect on relaxations to 2-methylthio ATP (3 nM-3 MicroM) in rabbit mesenteric artery and to ATP (1 MicroM-I mM) in rabbit aorta (with endothelium intact or removed). In addition,PPADS (30 MicroM) had no significant influence on the contractile potency of noradrenaline and histamine in rabbit ear and saphenous artery, respectively.5. In conclusion, these results support the evidence that PPADS is a selective antagonist of P2X-purinoceptor-mediated responses.
摘要
  1. 研究了P2嘌呤受体拮抗剂磷酸吡哆醛-6-偶氮苯-2',4'-二磺酸（PPADS）拮抗以下作用的能力：（1）α,β-亚甲基ATP（α,β-MeATP）或电场刺激（EFS）诱发的兔中耳动脉和隐动脉P2X嘌呤受体介导的收缩；（2）兔肠系膜动脉P2Y嘌呤受体介导的舒张；（3）兔主动脉内皮依赖性和非内皮依赖性P2Y嘌呤受体介导的舒张。2. α,β-MeATP（0.1 - 100 μM）引起兔耳动脉和隐动脉浓度依赖性收缩。在不存在PPADS时，产生相当于去甲肾上腺素（耳动脉）或组胺（隐动脉）EC25收缩作用的负对数[α,β-MeATP]在耳动脉和隐动脉中分别为6.60±0.18（9）和6.18±0.17（9）。PPADS（1 - 30 μM）浓度依赖性抑制外源性α,β-MeATP的这些作用。在耳动脉中，在1、3和10 μM的PPADS存在下，产生相当于去甲肾上腺素EC25收缩反应的负对数[α,β-MeATP]分别为6.16±0.18（8）、5.90±0.18（8）和4.72±0.36（8）（P < 0.01）。在隐动脉中，在1、3、10和30 μM浓度的PPADS存在下，相当于组胺EC25的负对数[α,β-MeATP]值分别为5.90±0.19（8）、5.73±0.16（8）、4.99±0.14（8）和4.51±0.13（8）（P < 0.01）。3. 1 μM浓度的PPADS对EFS（4 - 6频率；存在1 μM酚妥拉明）诱发的耳动脉收缩无影响。在较高浓度（3 - 30 μM）时，它引起神经源性收缩的浓度依赖性抑制。在隐动脉中，PPADS（1 - 30 μM）浓度依赖性抑制4、8和16 Hz频率的EFS诱发的收缩。仅在10和30 μM浓度时，PPADS才显著抑制32和64 Hz频率的EFS诱发的收缩。4. PPADS（30 μM）对兔肠系膜动脉中对2-甲硫基ATP（3 nM - 3 μM）和兔主动脉中对ATP（1 μM - 1 mM）（内皮完整或去除）的舒张无影响。此外，PPADS（30 μM）分别对兔耳动脉和隐动脉中去甲肾上腺素和组胺的收缩效能无显著影响。5. 总之，这些结果支持PPADS是P2X嘌呤受体介导反应的选择性拮抗剂这一证据。