Endoh M, Hillen B, Schümann H J
Arch Int Pharmacodyn Ther. 1977 Aug;228(2):213-21.
On the isolated papillary muscle of the rabbit the maximal developed tension induced by phenylephrine bia alpha-adrenoceptors was not affected by changing the temperature, while the basal developed tension of the muscle was significantly increased or decreased by lowering the temperature from 37 degrees C to 32 degrees C or by raising it to 42 degrees C, respectively. When the temperature was lowered from 37 degrees C to 32 degrees C in the muscle stimulated at a frequency of 0.5 Hz, the dose-response curve for phenylephrine via alpha-adrenoceptors was shifted to the left (delta pD2-0.47), while that for phenylephrine via beta-adrenoceptors was also shifted to the left to a similar extent (delta pD2=0.43). When the temperature was raised from 37 degrees C to 42 degrees C, the dose-response curve for phenylephrine via alpha-adrenoceptors was markedly shifted to the right (delta pD2=1.58), whereas that via beta-adrenoceptors was not affected at all by this elevation of the temperature (delta pD2=0.04). The change of the stimulation frequency affected chiefly the intrinsic activity of phenylephrine but not the affinity of the drug for alpha-adrenoceptors expressed as the pD2-value.
在兔离体乳头肌上,苯肾上腺素通过α-肾上腺素受体诱导的最大张力不受温度变化影响,而将温度从37℃降至32℃或升至42℃时,肌肉的基础张力分别显著升高或降低。当以0.5Hz频率刺激肌肉,温度从37℃降至32℃时,苯肾上腺素通过α-肾上腺素受体的剂量-反应曲线向左移动(ΔpD2 = 0.47),而苯肾上腺素通过β-肾上腺素受体的剂量-反应曲线也向左移动至类似程度(ΔpD2 = 0.43)。当温度从37℃升至42℃时,苯肾上腺素通过α-肾上腺素受体的剂量-反应曲线明显向右移动(ΔpD2 = 1.58),而通过β-肾上腺素受体的剂量-反应曲线则完全不受该温度升高的影响(ΔpD2 = 0.04)。刺激频率的变化主要影响苯肾上腺素的内在活性,但不影响以pD2值表示的药物对α-肾上腺素受体的亲和力。