Legrand C, Vivat V, Rigolot C, Maltier J P
Laboratoire de Physiologie de la Reproduction, CNRS URA 555, Université Pierre et Marie Curie, Paris, France.
J Pharmacol Exp Ther. 1991 Feb;256(2):767-72.
Receptor autoradiography using (-)-3-[125I]cyanopindolol and [3H]prazosin was used to study the distribution of beta and alpha-1 adrenoceptors in the rat uterus at early and midpregnancy. The binding of [3H]prazosin to slide-mounted sections at 25 degrees C was time dependent (K1 = 3.01 x 10(7) M-1 min-1, K2 = -0.0116 min-1) and saturable (1 nM). Competition binding curves with the selective alpha-1 and alpha-2 antagonists (prazosin, yohimbine) or alpha-1 and alpha-2 agonists (phenylephrine, clonidine) showed the presence of alpha-1 adrenoceptors; autoradiographic studies revealed that this subtype is highly localized in the circular layer of the myometrium during pregnancy. (-)-3-[125I]Cyanopindolol binding to slide-mounted sections of the pregnant uterus at 25 degrees C was time dependent (K1 = 4.68 x 10(8) M-1 min-1, K2 = -0.0117 min-1) and saturable (200 pM). Competition binding curves with beta-1 or beta-2 selective agonists (dobutamine, metaproterenol) and antagonists (atenolol, ICI 118,551) revealed the presence of beta adrenoceptors in the proportion of 67% beta-2 to 33% beta-1. Hyperfilm exposed to sections of the whole pregnant uterus incubated with (-)-3-[125I]cyanopindolol with or without ICI 118,551 or atenolol showed a high density of beta-2 adrenoceptors in the longitudinal layer of the myometrium and in the placenta. A small density of beta-2 adrenoceptors was also located in the decidua basalis on day 8 of pregnancy.
采用（-）-3-[¹²⁵I]氰胍心安和[³H]哌唑嗪进行受体放射自显影，研究妊娠早期和中期大鼠子宫中β和α-1肾上腺素能受体的分布。25℃下，[³H]哌唑嗪与载玻片上的切片结合具有时间依赖性（K1 = 3.01×10⁷ M⁻¹ min⁻¹，K2 = -0.0116 min⁻¹）且可饱和（1 nM）。与选择性α-1和α-2拮抗剂（哌唑嗪、育亨宾）或α-1和α-2激动剂（去氧肾上腺素、可乐定）的竞争结合曲线表明存在α-1肾上腺素能受体；放射自显影研究显示，该亚型在妊娠期间高度定位于子宫肌层的环形层。25℃下，（-）-3-[¹²⁵I]氰胍心安与妊娠子宫载玻片上的切片结合具有时间依赖性（K1 = 4.68×10⁸ M⁻¹ min⁻¹，K2 = -0.0117 min⁻¹）且可饱和（200 pM）。与β-1或β-2选择性激动剂（多巴酚丁胺、间羟异丙肾上腺素）和拮抗剂（阿替洛尔、ICI 118,551）的竞争结合曲线表明，β肾上腺素能受体中β-2与β-1的比例为67%比33%。用（-）-3-[¹²⁵I]氰胍心安孵育的整个妊娠子宫切片，无论有无ICI 118,551或阿替洛尔，曝光后的Hyperfilm显示子宫肌层纵行层和胎盘中β-2肾上腺素能受体密度较高。妊娠第8天，蜕膜基底层也有少量β-2肾上腺素能受体。
