Carneiro R C, Markus R P, Dubocovich M L
Department of Pharmacology, Northwestern University Medical School, Chicago, Ill. 60611.
Biol Signals. 1993 Jul-Aug;2(4):194-8.
To further understand the mechanism by which melatonin potentiates noradrenergic transmission in the rat vas deferens, we localized and partially characterized 2-[125I]-iodomelatonin-binding sites in tissue sections of the rat vas deferens using quantitative autoradiography. High-affinity 2-[125I]-iodomelatonin-binding sites were localized around the lumen of the prostatic portion, but not in the epididymal portion of the rat vas deferens. The binding of 2-[125I]-iodomelatonin to sections of the prostatic portion was stable, reversible and saturable. Saturation studies revealed a single class of high-affinity binding sites with a dissociation constant (Kd) of 104.2 +/- 23.7 pM (n = 4) and a binding capacity (Bmax) of 2.07 +/- 0.19 fmol/mg of protein (n = 4). These results suggest that melatonin may regulate sympathetic neurotransmission through activation of specific melatonin receptors in the prostatic portion of the rat vas deferens.
为了进一步了解褪黑素增强大鼠输精管去甲肾上腺素能传递的机制,我们使用定量放射自显影技术,在大鼠输精管组织切片中定位并部分表征了2-[¹²⁵I] - 碘褪黑素结合位点。高亲和力的2-[¹²⁵I] - 碘褪黑素结合位点定位于大鼠输精管前列腺部管腔周围,而附睾部则没有。2-[¹²⁵I] - 碘褪黑素与前列腺部切片的结合是稳定、可逆且可饱和的。饱和研究显示存在一类单一的高亲和力结合位点,解离常数(Kd)为104.2±23.7 pM(n = 4),结合容量(Bmax)为2.07±0.19 fmol/mg蛋白质(n = 4)。这些结果表明,褪黑素可能通过激活大鼠输精管前列腺部的特定褪黑素受体来调节交感神经传递。