Department of Pharmacodynamics, Jagiellonian University, Medical College, Faculty of Pharmacy, Medyczna 7, PL 30-688 Kraków, Poland.
Pharmacol Rep. 2009 Nov-Dec;61(6):1211-5. doi: 10.1016/s1734-1140(09)70186-0.
Local anesthetics (LAs) inhibit membrane depolarization by reducing sodium and potassium conductance, and subsequent displacement of calcium ions from binding sites seems to occur. Histamine release appears to be a secretory process in which calcium couples the stimulus to the exocytosis of histamine-containing granules. Furthermore, LAs are structurally similar to histamine H(1)-receptor antagonists. Thus, LAs can be considered antihistaminic drugs. Previous pharmacological investigations have shown strong local anesthetic, anti-inflammatory and analgesic activity of the carane derivative KP-23. As it has previously been demonstrated that KP-23R,S and its R,S-diasteroisomers have an inhibitory effect on guinea pig ileum contractions, the aim of the present study was to determine and compare the antihistaminic effects of KP-23R,S and its individual isomers KP-23R and KP-23S on isolated guinea pig ileum.
局部麻醉剂（LAs）通过降低钠和钾的通透性来抑制膜去极化，随后似乎会发生钙离子从结合位点的移位。组胺释放似乎是一种分泌过程，其中钙离子将刺激与含组胺颗粒的胞吐作用偶联。此外，LAs 在结构上与组胺 H(1)-受体拮抗剂相似。因此，LAs 可以被认为是抗组胺药物。先前的药理学研究表明，蒈烷衍生物 KP-23 具有很强的局部麻醉、抗炎和镇痛活性。由于先前已经证明 KP-23R,S 及其 R,S-非对映异构体对豚鼠回肠收缩具有抑制作用，因此本研究的目的是确定并比较 KP-23R,S 及其单个异构体 KP-23R 和 KP-23S 对分离的豚鼠回肠的抗组胺作用。
