Comparison of the effects of arylazido aminopropionyl ATP (ANAPP3), an ATP antagonist, on responses of the smooth muscle of the guinea-pig vas deferens to ATP and related nucleotides.
Comparison of the effects of arylazido aminopropionyl ATP (ANAPP3), an ATP antagonist, on responses of the smooth muscle of the guinea-pig vas deferens to ATP and related nucleotides.
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比较 ATP 拮抗剂芳基叠氮氨基丙酰 ATP (ANAPP3) 对豚鼠输精管平滑肌对 ATP 和相关核苷酸反应的影响。
DOI：
10.1016/0014-2999(82)90215-1
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发表时间：
1982
影响因子：
5
通讯作者：
O'Donnell,JP
中科院分区：
文献类型：
--
作者：
Fedan,JS;Hogaboom,GK;Westfall,DP;O'Donnell,JP
豚鼠输精管平滑肌对ATP和相关类似物的收缩反应以前曾被认为涉及刺激细胞表面P2-嘌呤能受体和强制性水解，这取决于核苷酸的浓度和结构。这一假设进一步测试通过评估的拮抗作用arylazido氨基丙酰ATP（ANAPP 3），一个特定的P2-嘌呤受体拮抗剂，浓度-反应关系和个人的个人资料，ATP和类似物含有磷酸链，核糖和腺嘌呤修饰。ATP、β，γ-亚甲基ATP（APPCP）、β，γ-亚氨基ATP（APPNP）和腺苷5′-O-（3-硫代三磷酸）（ATPγS）的浓度-反应曲线均为双峰型，表明存在两种受体，一种对腺嘌呤核苷酸具有高亲和力，一种对腺嘌呤核苷酸具有低亲和力。ANAPP 3处理后，观察到的拮抗作用类型为核苷酸特异性，浓度-反应曲线为单S形。对于ATP，在低浓度（< 3 × 10− 5 M）时拮抗作用最大，但不影响最大反应;对于APPCP和APPNP，在高浓度（> 3 × 10− 5 M）时拮抗作用最大，并导致最大反应降低;对于四磷酸腺苷（APPPP），在低浓度和高浓度时拮抗作用都很明显;对于ATPγS，在所有浓度下拮抗作用都是中等的。第二组效力较低的核苷酸的浓度-响应曲线是单S形的。包括ADP、α，β-亚甲基ADP（APCP）、8-溴ATP（8-BrATP）和2-脱氧ATP（2d-ATP）。用ANAPP 3处理使这些类似物的浓度-反应曲线向右移动，但没有降低最大反应。个体反应特征在结构上相关。对于大多数类似物，对低浓度核苷酸的反应是阶段性的和尖峰状的。ATP、ADP、ATPγS、APPPP和2d-ATP浓度升高时出现明显的紧张相。ANAPP 3拮抗反应的初始成分，但不影响紧张相。反应的初始阶段性成分与制剂的受体介导的刺激有关，而无5′-酸酐桥取代的核苷酸的特征性紧张成分似乎是由化合物的水解引发的，这是一个对ANAPP 3不敏感的过程。
Contractile responses of the smooth muscle of the guinea-pig vas deferens to ATP and related analogs have been suggested previously to involve stimulation of cell-surface P2-purinergic receptors and obligatory hydrolysis, depending on the concentration and structure of the nucleotide. This hypothesis was further tested by evaluating the antagonistic effect of arylazido aminopropionyl ATP (ANAPP3), a specific P2-purinergic receptor antagonist, on concentration-response relationships and on the profiles of individual responses to ATP and analogs containing phosphate-chain, ribose and adenine modifications. The concentration-response curves for ATP, β, γ-methylene ATP (APPCP), β, γ-imido ATP (APPNP) and adenosine 5′-O-(3-thiotriphosphate) (ATPγS) were bimodal and suggested the existence of two receptors, one with high and one with low affinity for adenine nucleotides. The type of antagonism observed was nucleotide-specific, and concentration-response curves were monosigmoidal after ANAPP3treatment. For ATP, antagonism was greatest at low concentrations (< 3 × 10−5M) and did not affect the maximum response; for APPCP and APPNP, it was greatest at high concentrations (> 3 × 10−5M) and resulted in a reduction in maximum response; for adenosine tetraphosphate (APPPP) the antagonism was pronounced at low and high concentrations; for ATPγS the antagonism was moderate at all concentrations. The concentration-response curves for a second group of less potent nucleotides was monosigmoidal. Included in this group was ADP, α, β-methylene ADP (APCP), 8-bromo ATP (8-BrATP) and 2-deoxy ATP (2d-ATP). Treatment with ANAPP3shifted the concentration-response curves for these analogs to the right but did not reduce maximum responses. The characteristics of individual response profiles were structurally related. For most analogs responses to low concentrations of nucleotides were phasic and spike-like. Discernible tonic phases appeared with higher concentrations of ATP, ADP, ATPγS, APPPP and 2d-ATP. ANAPP3antagonized the initial component of responses but did not affect the tonic phase. The initial phasic component of response has been related to receptor-mediated stimulation of the preparations, while the tonic component, characteristic of nucleotides without 5′-anhydride bridge substitutions, appears to be initiated by hydrolysis of the compounds, a process which is insensitive to ANAPP3.
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腺苷 5â2-0(3-硫代三磷酸) 控制磷酸酶活性â
DOI：
--
发表时间：
1974
期刊：
影响因子：
--
作者：
D. Gratecos;E. Fischer
通讯作者：
E. Fischer
DOI：
--
发表时间：
1981
期刊：
影响因子：
--
作者：
G. Burnstock;Christine M. Brown
通讯作者：
Christine M. Brown
腺苷-α、β-亚甲基二磷酸对肠平滑肌的作用：作用位点和可能的前列腺素参与。
影响因子：
3.5
作者：
R. Frew;H. Baer
通讯作者：
H. Baer
鸡肫：钙激活磷酸化与收缩的关系。
影响因子：
56.9
作者：
P. E. Hoar;W. Kerrick;P. Cassidy
通讯作者：
P. Cassidy
肝质膜中两个α-肾上腺素能结合位点的证据。
影响因子：
4.8
作者：
M. El;P. Blackmore;J. Exton
通讯作者：
J. Exton