Gibson A, Samini M
J Pharm Pharmacol. 1979 Dec;31(12):826-30. doi: 10.1111/j.2042-7158.1979.tb13674.x.
Noradrenaline (NA) and dopamine (DA) contracted the mouse vas deferens and reduced the responses to low frequency nerve stimulation (0.1 Hz). The relative potencies of antagonists suggested that these effects were due to stimulation of post-synaptic and pre-synaptic alpha-adrenoceptors respectively. Bromocriptine produced a non-competitive antagonism of contractile responses to NA (pD2' = 7.6) and DA (pD2' = 8.0) but had no effect on responses to carbachol. Bromocriptine also reduced single twitch responses of the vas to low frequency field stimulation (0.1 Hz), but did not affect stimulation at higher frequencies (1--20 Hz). Yohimbine selectively and rapidly reversed the inhibiting effects of bromocriptine on single twitches, although they could not easily be reversed by washing. Bromocriptine produced a yohimbine-reversible reduction in the stimulated overflow of tritium from vasa previously loaded with 3H--NA. Thus the mouse vas deferens does not appear to contain specific DA receptors and the results suggest that bromocriptine acts as a pre-synaptic alpha-adrenoceptor agonist and post-synaptic alpha-adrenoceptor antagonist in this tissue.
去甲肾上腺素(NA)和多巴胺(DA)使小鼠输精管收缩,并降低了对低频神经刺激(0.1Hz)的反应。拮抗剂的相对效价表明,这些作用分别是由于对突触后和突触前α-肾上腺素能受体的刺激所致。溴隐亭对NA(pD2' = 7.6)和DA(pD2' = 8.0)的收缩反应产生非竞争性拮抗作用,但对卡巴胆碱的反应无影响。溴隐亭还降低了输精管对低频场刺激(0.1Hz)的单收缩反应,但不影响高频(1-20Hz)刺激。育亨宾选择性且迅速地逆转了溴隐亭对单收缩的抑制作用,尽管通过冲洗不易逆转。溴隐亭使先前加载有3H-NA的输精管中受刺激的氚溢出量产生育亨宾可逆性减少。因此,小鼠输精管似乎不含有特异性DA受体,结果表明溴隐亭在该组织中充当突触前α-肾上腺素能受体激动剂和突触后α-肾上腺素能受体拮抗剂。