Beding-Barnekow B, Leander S, Ohlin M, Ninn-Pedersen K, Alkner U, Håkanson R
Department of Pharmacology, Lund University, Sweden.
Exp Eye Res. 1990 Jan;50(1):21-6. doi: 10.1016/0014-4835(90)90006-g.
Previous observations have indicated that topical application to the rabbit eye of tachykinin antagonists, including spantide, effectively prevents the miosis and the disruption of the blood-aqueous barrier consequent to ocular injury. The present study shows that spantide is taken up into the rabbit eye following topical application. This was established by determination of spantide in the aqueous humor by radioimmunoassay. The concentrations reached in the aqueous humor were those that could be expected to block tachykinin receptors. The elimination of spantide from the aqueous humor was found to be slow. From HPLC analysis it seemed that spantide in the aqueous humor is degraded to smaller products, predominantly spantide 5-11. Some of the topically applied peptide appeared in the general circulation. Here the rate of elimination was rapid by comparison. Very small amounts of spantide appeared in the cerebrospinal fluid after intravenous injection.
先前的观察表明，将速激肽拮抗剂（包括spantide）局部应用于兔眼，可有效预防眼损伤后随之而来的瞳孔缩小和血-房水屏障破坏。本研究表明，局部应用后spantide可被兔眼吸收。这是通过放射免疫分析法测定房水中的spantide来确定的。房水中达到的浓度是预期能够阻断速激肽受体的浓度。发现spantide从房水中消除缓慢。从高效液相色谱分析来看，房水中的spantide似乎降解为较小的产物，主要是spantide 5-11。一些局部应用的肽出现在体循环中。相比之下，这里的消除速度很快。静脉注射后，脑脊液中出现的spantide量极少。
