牛脑微血管平滑肌细胞上特异的白三烯C_4受体

Specific |3H|LTC4 Receptors on Intact Smooth Muscle Gells Derived from Bovine Cerebral Microvasculatures

作者鉴定了培养的牛脑微血管平滑肌细胞上特异的白三烯C_4(LTC_4)受体。[~3H]LTC_4与该细胞的结合在25℃时具有快速、饱和及可逆的特点。随着[~3H]LTC_4浓度的增加,[~3H]LTC_4与细胞的特异结合也增加,最后达到坪值。Scatchard作图表明[~3H]LTC_4与上述细胞只有一个结合位点,其K_d=2.01±0.4nmol/L,B_(max)=156.6±13.1fmol/10~6细胞,这种结合可被未标记的LTC_4,LTD_4和FPL-55712抑制,在10^(-5)mol/L时,三者的抑制率分别是96.9％,73.9％和44.9％。

Specific receptors for leukotriene C4 LTC4 have been identified on intact smooth muscle cells derived from bovine cerebral microvasculatures. Specific pHJLTC4, binding at a fixed input at 25 ℃ was rapid , reaching the maximum at 20min With incremental inputs of radioligand and a constant cell number, specific [3H]LTC4 binding reached a plateau indicative of a saturable binding site. Analysis of Scatchard plots demonstrated a single high affinity binding site with a dissociation constant (Kd) of 2.01±0.4 nmol/L and Bmax = 156.6±13.1 fmol/106 cells. The specific [3H]LTC4 binding could be inhibited by unlabted LTC4, LTD4 and FPL-55712 with an inhibitory rate of 96.9%, 73.9% and 44.9% at 10-5 mol/L, respectively.