Larsson B, Sjögren C, Andersson K E
Acta Physiol Scand. 1986 Jan;126(1):39-43. doi: 10.1111/j.1748-1716.1986.tb07786.x.
The aim of the present investigation was to study the regional distribution of alpha-adrenoceptor subtypes in the female rabbit bladder base and urethra, using radioligand binding and mechanical activity studies. The binding studies performed on membranes prepared from the bladder base, and the proximal and distal part of the urethra, revealed that the number of alpha 1-adrenoceptors did not significantly differ between the three regions, whereas the number of alpha 2-adrenoceptors increased distally. The mechanical activity studies showed that noradrenaline and clonidine, but not phenylephrine, were more potent in the distal than the proximal part of the urethra. It is suggested that in the female rabbit urethra the lower EC50-value found for noradrenaline and clonidine in the distal as compared to the proximal part of the urethra, at least in part, is attributable to a higher number of postjunctional alpha 2-adrenoceptors in the distal than in the proximal urethra.
本研究的目的是利用放射性配体结合和机械活性研究,探讨雌性兔膀胱底部和尿道中α-肾上腺素能受体亚型的区域分布。对从膀胱底部以及尿道近端和远端制备的膜进行的结合研究表明,α1-肾上腺素能受体的数量在这三个区域之间没有显著差异,而α2-肾上腺素能受体的数量在远端增加。机械活性研究表明,去甲肾上腺素和可乐定(而非苯肾上腺素)在尿道远端比近端更有效。提示在雌性兔尿道中,与近端相比,去甲肾上腺素和可乐定在远端的较低半数有效浓度(EC50)值,至少部分归因于远端比近端尿道中更多的节后α2-肾上腺素能受体。