Calcutt C R, Ganellin C R, Jackson B, Leigh B K, Owen D A, Smith I R
Eur J Pharmacol. 1987 Jan 6;133(1):65-74. doi: 10.1016/0014-2999(87)90206-8.
Competition by the potent selective H1-receptor antagonist temelastine (SK & F 93944) with [3H]mepyramine binding to mouse cortex H1-receptors has been measured in vitro and vivo. The data were compared with that obtained using the classical H1-receptor antagonists mepyramine and promethazine and indicated that temelastine has relatively low ability to penetrate the blood-brain barrier compared with the latter two compounds. These studies also revealed that temelastine has relatively low affinity for mouse cortex H1-receptors compared with its affinity for H1-receptors in guinea-pig ileum and cortex, suggesting that it may be a useful compound with which to investigate potential H1-receptor tissue and species-related differences.
强效选择性H1受体拮抗剂替美斯汀（SK&F 93944）与[3H]美吡拉敏结合小鼠皮质H1受体的竞争作用已在体外和体内进行了测定。将这些数据与使用经典H1受体拮抗剂美吡拉敏和异丙嗪获得的数据进行比较，结果表明，与后两种化合物相比，替美斯汀穿透血脑屏障的能力相对较低。这些研究还表明，与豚鼠回肠和皮质中的H1受体相比，替美斯汀对小鼠皮质H1受体的亲和力相对较低，这表明它可能是一种用于研究潜在H1受体组织和物种相关差异的有用化合物。
