Regulation of muscarinic receptor binding by guanine nucleotides and N-ethylmaleimide.
Regulation of muscarinic receptor binding by guanine nucleotides and N-ethylmaleimide.
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鸟嘌呤核苷酸和 N-乙基马来酰亚胺对毒蕈碱受体结合的调节。
DOI：
10.1002/jss.400140204
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发表时间：
1980
期刊：
影响因子：
--
通讯作者：
Yamamura,HI
中科院分区：
文献类型：
--
作者：
Ehlert,FJ;Roeske,WR;Yamamura,HI
用[~3H]顺式甲基二氧戊环([~3H]Cd)作为激动剂，研究了鸟苷和N-乙基马来酰亚胺(NEM)对M受体结合的调节作用。对大鼠前脑匀浆的特性研究表明，[~3H]Cd结合与组织浓度呈线性关系，不受pH从5.5到8.0的变化的影响。大鼠脑内[~3H]Cd结合量的区域性变化与[~3H](−)-3-喹诺基苯甲酸酯([~3H](−)QNb)结合量的变化大体相关，尽管结合的绝对变化较小。在100μM浓度下，鸟苷类似物5‘-基亚胺二磷酸[GPP(NH)p]对纹状体、回肠和心脏的[~3H]Cd结合抑制43-77%。用几种浓度的GPP(NH)p进行结合研究的结果表明，该鸟嘌呤核苷酸抑制[~3H]Cd结合的效力在心脏比在回肠更强。与之相反，GPP(NH)p使心脏和回肠的[~3H](−)qNb结合量增加，而纹状体区的[~3H](−)qNb结合量无变化。GPP(NH)p(100μM)竞争性抑制与回肠纵肌结合的[~3H](GPP)QNb，引起一系列激动剂的IC50值增加，其作用与这些化合物的药效有关。NEM处理的前脑匀浆的结合研究结果表明，NEM能增强[~3H]Cd的结合。
The regulation of muscarinic receptor binding by guanine nucleotides and N‐ethylmaleimide (NEM) was investigated using the agonist ligand, [3H] cis methyldioxolane ([3H] CD). Characterization studies on rat forebrain homogenates showed that [3H] CD binding was linear with tissue concentration and was unaffected by a change in pH from 5.5 to 8.0. The regional variation in [3H] CD binding in the rat brain correlated generally with [3H] (−)3‐quinuclidinyl benzilate ([3H] (−)QNB) binding, although the absolute variation in binding was somewhat less. At a concentration of 100 μM, the GTP analogue, guanyl‐5′‐yl imidodiphosphate [Gpp(NH)p], caused a 43–77% inhibition of [3H] CD binding in the corpus striatum, ileum, and heart. The results of binding studies using several Gpp(NH)p concentrations demonstrated that the potency of this guanine nucleotide for inhibition of [3H] CD binding was greater in the heart than in the ileum. In contrast to its effects on [3H] CD binding, Gpp(NH)p caused an increase in [3H] (−)QNB binding in the heart heart and ileum and no change in [3H] (−)QNB binding in the corpus striatum. When measured by competitive inhibition of [3H] (−)QNB binding to the longitudinal muscle of the ileum, Gpp(NH)p (100 μM) caused an increase in the IC50values of a series of agonists in a manner that was correlated with the efficacy of these compounds. The results of binding studies on NEM treated forebrain homogenates revealed an enhancement of [3H] CD binding by NEM.
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激动剂与脑毒蕈碱受体的结合。
影响因子：
3.6
作者：
N. Birdsall;A. Burgen;E. Hulme
通讯作者：
E. Hulme
鸟苷基-5-基亚胺二磷酸和钠对大鼠脑和大鼠回肠纵肌中毒蕈碱受体结合的影响。
影响因子：
6.1
作者：
F. Ehlert;W. Roeske;L. Rosenberger;H. Yamamura
通讯作者：
H. Yamamura
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影响因子：
3.9
作者：
H. Pollard
通讯作者：
H. Pollard
使用激动剂[3H]顺式甲基二氧戊环在大鼠脑中结合毒蕈碱受体。
影响因子：
6.1
作者：
F. Ehlert;Y. Dumont;W. Roeske;H. Yamamura
通讯作者：
H. Yamamura
毒蕈碱乙酰胆碱受体相互作用：激动剂和拮抗剂的竞争结合研究
影响因子：
2.9
作者：
Y. Kloog;M. Sokolovsky
通讯作者：
M. Sokolovsky