Activation of adenosine A1 receptor by N6-(R)-phenylisopropyladenosine (R-PIA) inhibits forskolin-stimulated tyrosine hydroxylase activity in rat striatal synaptosomes.
Activation of adenosine A1 receptor by N6-(R)-phenylisopropyladenosine (R-PIA) inhibits forskolin-stimulated tyrosine hydroxylase activity in rat striatal synaptosomes.
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N6-(R)-苯基异丙基腺苷 (R-PIA) 激活腺苷 A1 受体可抑制大鼠纹状体突触体中毛喉素刺激的酪氨酸羟化酶活性。
DOI：
10.1016/0024-3205(90)90127-d
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发表时间：
1990
期刊：
影响因子：
6.1
通讯作者：
P. Onali
中科院分区：
文献类型：
--
作者：
M. Olianas;P. Onali
我们研究了相对选择性的A1腺苷受体激动剂N6-(R)-苯基异丙基腺苷(R-PIA)对大鼠纹状体突触体内酪氨酸羟基酶活性(TH)的影响。对用受试化合物预孵育的组织进行超声和离心后获得的上清液中的TH活性进行检测。R-PIA对基础酶有轻微的抑制作用，但对腺苷环化酶激动剂福司可林(FSK)的亚最大浓度(0.1~0.5μM)有显著抑制作用。R-PIA的IC50值为17 nM，最大抑制值对应于FSK刺激的酶活性下降30-40%。在对照和刺激条件下，PIA的S异构体均不影响TH活性。腺苷受体阻断剂8-环戊基-1，3-二甲基黄嘌呤可完全拮抗R-PIA的抑制作用。R-PIA抑制基础和FSK刺激的腺苷环化酶活性。这些结果表明，纹状体多巴胺能终末的TH活性可以通过激活突触前A1腺苷受体而被抑制地调节。
We investigated the effect of the relatively selective A1 adenosine receptor agonist N6-(R)-phenylisopropyladenosine (R-PIA) on tyrosine hydroxylase activity (TH) of synaptosomes obtained from rat striatum. TH activity was assayed in supernatant obtained following sonication and centrifugation of the tissue preincubated with the test compounds. R-PIA produced a modest decrease of basal enzyme activity, but significantly reduced the activation of the enzyme by submaximal (0.1–0.5 μM) concentrations of forskolin (FSK) a stimulator of adenylate cyclase. The IC 50 value of R-PIA was 17 nM and the maximal inhibition corresponded to 30–40% decrease of the enzyme activity stimulated by FSK. The S-isomer of PIA failed to affect TH activity under control and stimulated conditions. Moreover, the inhibitory effect of R-PIA was completely antagonized by 8-cyclopentyl- 1,3 -dimethylxanthine, an adenosine receptor blocker. R-PIA inhibited both basal and FSK-stimulated adenylate cyclase activity. These results indicate that in striatal dopaminergic terminals TH activity can be modulated in an inhibitory manner by activation of presynaptic A1 adenosine receptors.
DOI：
10.1016/s0021-9258(18)33559-2
发表时间：
1982-11
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
J. Haycock;J. Meligeni;W. Bennett;J. Waymire
通讯作者：
J. Haycock;J. Meligeni;W. Bennett;J. Waymire
多巴胺自身受体对纹状体酪氨酸羟化酶动力学状态的调节。
影响因子：
3.6
作者：
Strait,KA;Kuczenski,R
通讯作者：
Kuczenski,R
腺苷受体激动剂抑制大鼠纹状体切片中磷酸肌醇的积累。
影响因子：
5
作者：
Petcoff,DW;Cooper,DM
通讯作者：
Cooper,DM