Effects of cooling on alpha-1-adrenoceptor mechanisms in rat aorta.

I Takayanagi, K Koike, M Nakamura, Y Horie
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Abstract

1. The effects of cooling from 37 degrees C to 25 degrees C on alpha-1-adrenoceptor mechanisms in isolated rat aortic strips were studied. 2. The dissociation constant and the maximum binding for [3H]-prazosin, and the pA2-values (negative logarithm of dissociation constant) of clonidine and prazosin against noradrenaline were not influenced by cooling. 3. These results indicate that cooling did not influence the affinity of a competitive antagonist and receptor concentration. 4. Cooling increased the dissociation constant of noradrenaline but decreased its efficacy. 5. A receptor occupancy-response curve for noradrenaline was a rectangular hyperbola at 37 degrees C but linear at 25 degrees C, suggesting that a relationship between the contractile response and receptor occupancy was changed by cooling.

冷却对大鼠主动脉α -1肾上腺素能受体机制的影响。
1. 研究了37℃~ 25℃冷却对大鼠离体主动脉条α -1-肾上腺素能受体机制的影响。2. [3H]-prazosin的解离常数和最大结合,以及可乐定和prazosin对去甲肾上腺素的pa2值(解离常数的负对数)不受冷却的影响。3.这些结果表明,冷却不影响竞争性拮抗剂和受体浓度的亲和力。4. 降温使去甲肾上腺素的解离常数升高,但降低了其药效。5. 去甲肾上腺素的受体占用-反应曲线在37℃时呈矩形双曲线,而在25℃时呈线性,表明收缩反应和受体占用之间的关系随着冷却而改变。
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