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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Reilly M P, Horiuchi K, Asakura T

Division of Hematology, Children's Hospital of Philadelphia, PA 19104.

Gen Pharmacol. 1993 Nov;24(6):1323-9. doi: 10.1016/0306-3623(93)90414-s.

Bepiridil, (beta-[(2-methylpropoxy)methyl]-N-phenyl-N-(phenyl-methyl)-1-py rro lidine-ethanamine), a calcium channel blocker, inhibits sickling of red blood cells (RBC) from patients with sickle cell disease (SCD) at micromolar concentrations in vitro. 2. Bepridil induces dose-dependent osmotic swelling of RBC and a concomitant decrease in mean corpuscular hemoglobin concentration (MCHC). 3. Modest decreases in MCHC greatly lengthen the delay time for polymerization of deoxygenated sickle hemoglobin (Hb S) and inhibit RBC sickling. 4. Equilibrium dialysis studies of bepridil and purified hemoglobin showed a low binding affinity (Kb = 10(3)/M). 5. The partition coefficient (Kp) determined for the interaction of RBC and bepridil was 1-3 x 10(3), which is similar to the Kp determined for other amphipathic molecules, such as chlorpromazine.

苄普地尔，（β-[(2-甲基丙氧基)甲基]-N-苯基-N-(苯基甲基)-1-吡咯烷乙胺），一种钙通道阻滞剂，在体外微摩尔浓度下可抑制镰状细胞病（SCD）患者红细胞（RBC）的镰变。2. 苄普地尔诱导RBC剂量依赖性渗透肿胀，并伴随平均红细胞血红蛋白浓度（MCHC）降低。3. MCHC适度降低可显著延长去氧镰状血红蛋白（Hb S）聚合的延迟时间并抑制RBC镰变。4. 苄普地尔与纯化血红蛋白的平衡透析研究显示结合亲和力较低（Kb = 10³/M）。5. 测定的RBC与苄普地尔相互作用的分配系数（Kp）为1 - 3×10³，这与为其他两亲性分子（如氯丙嗪）测定的Kp相似。

Reilly M P, Horiuchi K, Asakura T

Division of Hematology, Children's Hospital of Philadelphia, PA 19104.

Gen Pharmacol. 1993 Nov;24(6):1323-9. doi: 10.1016/0306-3623(93)90414-s.

Bepiridil, (beta-[(2-methylpropoxy)methyl]-N-phenyl-N-(phenyl-methyl)-1-py rro lidine-ethanamine), a calcium channel blocker, inhibits sickling of red blood cells (RBC) from patients with sickle cell disease (SCD) at micromolar concentrations in vitro. 2. Bepridil induces dose-dependent osmotic swelling of RBC and a concomitant decrease in mean corpuscular hemoglobin concentration (MCHC). 3. Modest decreases in MCHC greatly lengthen the delay time for polymerization of deoxygenated sickle hemoglobin (Hb S) and inhibit RBC sickling. 4. Equilibrium dialysis studies of bepridil and purified hemoglobin showed a low binding affinity (Kb = 10(3)/M). 5. The partition coefficient (Kp) determined for the interaction of RBC and bepridil was 1-3 x 10(3), which is similar to the Kp determined for other amphipathic molecules, such as chlorpromazine.

苄普地尔，（β-[(2-甲基丙氧基)甲基]-N-苯基-N-(苯基甲基)-1-吡咯烷乙胺），一种钙通道阻滞剂，在体外微摩尔浓度下可抑制镰状细胞病（SCD）患者红细胞（RBC）的镰变。2. 苄普地尔诱导RBC剂量依赖性渗透肿胀，并伴随平均红细胞血红蛋白浓度（MCHC）降低。3. MCHC适度降低可显著延长去氧镰状血红蛋白（Hb S）聚合的延迟时间并抑制RBC镰变。4. 苄普地尔与纯化血红蛋白的平衡透析研究显示结合亲和力较低（Kb = 10³/M）。5. 测定的RBC与苄普地尔相互作用的分配系数（Kp）为1 - 3×10³，这与为其他两亲性分子（如氯丙嗪）测定的Kp相似。