大鼠大脑皮层中拮抗剂与毒蕈碱受体结合亲和力常数的温度系数
Temperature coefficients of affinity constants for the binding of antagonists to muscarinic receptors in the rat cerebral cortex.
作者信息
Barlow R B, Birdsall N J, Hulme E C
出版信息
Br J Pharmacol. 1979 Aug;66(4):587-90. doi: 10.1111/j.1476-5381.1979.tb13698.x.
Abstract
1 The temperature coefficients of binding of a series of muscarinic antagonists to their receptors in membrane preparations from the rat cerebral cortex has been examined. 2 At 37 degrees C the affinity constants agree with those determined by antagonism of acetylcholine-induced contractions of the guinea-pig ileum. 3 The temperature-dependence of the affinity constants is low; for the antagonists examined, the affinity constants at 0 degrees C differ by less than a factor of 3 from those measured at 37 degrees C. 4 There are qualitative similarities between the estimates of the temperature coefficient of binding of the antagonists to receptors in ileum strips and in the cerebral cortex.
摘要
- 已经研究了一系列毒蕈碱拮抗剂与大鼠大脑皮层膜制剂中其受体结合的温度系数。2. 在37℃时，亲和常数与通过拮抗乙酰胆碱诱导的豚鼠回肠收缩所测定的常数一致。3. 亲和常数的温度依赖性较低；对于所研究的拮抗剂，0℃时的亲和常数与37℃时测得的亲和常数相差不到3倍。4. 在回肠条和大脑皮层中，拮抗剂与受体结合的温度系数估计值在质量上有相似之处。
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A comparison of affinity constants for muscarine-sensitive acetylcholine receptors in guinea-pig atrial pacemaker cells at 29 degrees C and in ileum at 29 degrees C and 37 degrees C.豚鼠心房起搏细胞在29℃时以及回肠在29℃和37℃时毒蕈碱敏感性乙酰胆碱受体亲和常数的比较。
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