Wiik P
Norwegian Defence Research Establishment, Division for Environmental Toxicology, Kjeller.
Regul Pept. 1988 Apr;20(4):323-33. doi: 10.1016/0167-0115(88)90067-5.
The effect of agonists on VIP receptor regulation has been investigated in mononuclear human blood leucocytes. VIP receptor number and affinity, as well as VIP-stimulated cyclic AMP accumulation were measured after pretreatment with VIP, PHM-27 or secretin. Pretreatment for 30 min with 0.1 microM VIP caused 28% (S.E.M. = 15) reduction in specific binding, and 52% (S.E.M. = 12) reduction in cyclic AMP accumulation, while 3 h of pretreatment caused 59% (S.E.M. = 10) and 68% (S.E.M. = 12) reduction. Only VIP concentrations at the nanomolar level and higher were shown to have any effect. Bmax of the high-affinity receptor was reduced by 66% (S.E.M. = 8) after 30 min, and 95% (S.E.M. = 3) after 3 h of exposure to 0.1 microM VIP. No significant change was observed in receptor affinity, in Bmax of the low-affinity receptor, in ED50, or in ED100 of VIP-stimulated cyclic AMP accumulation. Pretreatment with PHM-27 (0.1 microM, 3 h) caused 24% reduction in [125I]VIP binding and 25% reduction in cyclic AMP accumulation, while no effect was detected after pretreatment with secretin (0.1 microM, 3 h).
已在人单核白细胞中研究了激动剂对血管活性肠肽（VIP）受体调节的影响。在用VIP、PHM - 27或促胰液素预处理后，测定了VIP受体数量、亲和力以及VIP刺激的环磷酸腺苷（cAMP）积累。用0.1微摩尔/升VIP预处理30分钟导致特异性结合减少28%（标准误=15），cAMP积累减少52%（标准误=12），而预处理3小时导致减少59%（标准误=10）和68%（标准误=12）。仅显示纳摩尔及更高浓度的VIP有任何作用。暴露于0.1微摩尔/升VIP 30分钟后，高亲和力受体的最大结合容量（Bmax）降低了66%（标准误=8），3小时后降低了95%（标准误=3）。在受体亲和力、低亲和力受体的Bmax、VIP刺激的cAMP积累的半数有效剂量（ED50）或完全有效剂量（ED100）方面未观察到显著变化。用PHM - 27（0.1微摩尔/升，3小时）预处理导致[125I]VIP结合减少24%，cAMP积累减少25%，而用促胰液素（0.1微摩尔/升，3小时）预处理后未检测到作用。
