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Characterization of the pharmacological profile of the potent LTB4 antagonist CP-105,696 on murine LTB4 receptors in vitro.

机译：在体外对强效LTB4拮抗剂CP-105,696对鼠LTB4受体的药理作用进行表征。

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1. Binding of [3H]-leukotriene B4 ([3H]-LTB4) to murine spleen membranes (MSM) was determined. 2. Scatchard analyses of [3H]-LTB4 binding indicated the presence of high (KD1 = 1.7 nM) and low (KD2 = 7.5 nM) affinity receptors on MSM with Bmax values of 151 fmol mg-1 protein (Bmax1) and 354 fmol mg-1 protein (Bmax2), respectively. 3. CP-105,696, a potent LTB4 antagonist, inhibited [3H]-LTB4 (0.67 nM) binding to the high affinity receptor on MSM, IC50 = 30.2 nM, Ki = 17.7 nM with a Hill coefficient of 0.93. 4. Scatchard analyses of [3H]-LTB4 binding to MSM in the presence of CP-105,696 indicated that the high-affinity receptor was inhibited in a non-competitive manner and the low-affinity receptor in a competitive manner. 5. Isolated peripheral blood murine neutrophils (MN) responded chemotactically to LTB4, EC50 = 2.5 nM. CP-105,696 blocked this response, IC50 = 2.3 nM. When examined over a full concentration-response range of LTB4, CP-105,696 inhibited chemotaxis in a non-competitive manner. 6. Murine neutrophils in anticoagulated whole blood upregulated the integrin, complement receptor type 3 (CD11b/CD18, Mac-1) in response to LTB4, EC50 = 20 nM and this was inhibited by CP-105,696 in a competitive manner. 7. These results provide evidence that MSM have specific binding sites for LTB4, and as exemplified by CP-105,696, that these receptors may be useful for determining the potency and nature of antagonism of novel LTB4 receptor antagonists.
机译：1.确定[3H]-白三烯B4（[3H] -LTB4）与鼠脾膜（MSM）的结合。 2. [3H] -LTB4结合的Scatchard分析表明MSM上存在高（KD1 = 1.7 nM）和低（KD2 = 7.5 nM）亲和力受体，Bmax值为151 fmol mg-1蛋白（Bmax1）和354 fmol mg-1蛋白（Bmax2）。 3. CP-105,696，一种有效的LTB4拮抗剂，抑制[3H] -LTB4（0.67 nM）与MSM上的高亲和力受体结合，IC50 = 30.2 nM，Ki = 17.7 nM，希尔系数为0.93。 4.在CP-105,696存在下对[3H] -LTB4与MSM结合的Scatchard分析表明，高亲和力受体以非竞争性方式被抑制，而低亲和力受体以竞争性方式被抑制。 5.分离的外周血鼠中性粒细胞（MN）对LTB4趋化性反应，EC50 = 2.5 nM。 CP-105,696阻止了​​此响应，IC50 = 2.3 nM。在LTB4的整个浓度响应范围内检查时，CP-105696以非竞争性方式抑制趋化性。 6.抗凝全血中的鼠中性粒细胞响应LTB4，EC50 = 20 nM上调了整联蛋白3型补体受体（CD11b / CD18，Mac-1），并且被竞争性地被CP-105696抑制。 7.这些结果提供了证据，证明MSM具有LTB4的特异性结合位点，如CP-105,696所示，这些受体可用于确定新型LTB4受体拮抗剂的拮抗作用和性质。

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