French A M, Scott N C
Br J Pharmacol. 1983 Dec;80(4):655-61. doi: 10.1111/j.1476-5381.1983.tb10055.x.
Graded contractile responses of the rat vas deferens were obtained to trains containing varying numbers of pulses delivered transmurally at 500 Hz, allowing construction of pulse-response curves. In the presence of postjunctional adrenoceptor blocking drugs, these curves were displaced to the right in a parallel manner, allowing the estimation of pA2 values for the drugs. Activity of drugs at prejunctional adrenoceptors was estimated from the reduction of inhibition of the response to a second pulse delivered 3 s after trains containing different numbers of pulses. It is suggested that the technique is more physiological than others used to determine the antagonistic activity of drugs at adrenoceptors.
在500Hz频率下经壁施加含有不同脉冲数的串刺激,可获得大鼠输精管的分级收缩反应,从而构建脉冲-反应曲线。在存在节后肾上腺素能受体阻断药物的情况下,这些曲线以平行方式向右移位,由此可估算药物的pA2值。通过含有不同脉冲数的串刺激后3秒施加的第二个脉冲反应抑制的降低,来估算药物在节前肾上腺素能受体的活性。有人认为,该技术比用于测定药物对肾上腺素能受体拮抗活性的其他技术更具生理性。