1995 Fiscal Year Final Research Report Summary
A STUDY ON THE BINDIND MODE OF LOCAL ANESTHETICS WITH PHOSPHOLIPID BILAYER AND SODIUM CHANNEL.
| Project/Area Number |
06454570
|
|---|
| Research Category |
Grant-in-Aid for General Scientific Research (B)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
Surgical dentistry
|
|---|
| Research Institution | HEALTH SCIENCES UNIVERSITY OF HOKKAIDO |
|---|
Principal Investigator |
KOKUBU Masahiro DEPARTMENT OF DENTAL ANESTHESIOLOGY,SCHOOL OF DENTISTRY,HEALTH SCIENCES UNIVERSITY OF HOKKAIDO.ASSOCIATE PROFESSOR., 歯学部, 助教授 (70124691)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
ODA Kazukaki SCHOOL OF PHARMACEUTICAL SCIENCES,HEALTH SCIENCES UNIVERSITY OF HOKKAIDO.ASSISTA, 薬学部, 助手 (80094829)
|
|---|
| Project Period (FY) |
1994 – 1995
|
| Keywords | LOCAL ANESTHETICS / SODIUM ION CHANNEL / ACTION MECHANISM / BINDIND SITES / PHOSPHOLIPID MEMBRANE / NMR Spectroscopy |
|---|
| Research Abstract |
The site of local anesthetics action is well known to be sodium channel. However, several questions have been raised in response to Hille's theory that specific receptor exist for local anesthetics. Local anesthetics can inhibit the passage of the sodium ion by binding to the biomembrane that surrouds the sodium channel, thereby altering the comformation of channel proteins and expressing their pharmacological effect. In this study, NMR was utilized to measure the binding ability of local anesthetics with the phospholipid membrane in order to compare the pharmacological characteristics (potency and toxity) of the anesthetics. The results of the study demonstrate that chemical shift values and the broadening of the choline methyl signal of phospholipid membrane are closely related and that the change of choline methyl signal in the membrane is useful indicator of proximity between the membrane and anesthetics. The results of the study also indicate that the binding ability of local anesthetics toward the phospholipid membrane was found to be directly proportional to the anesthetics potency, suggesting that the biomembrane plays an important role in the action mechanism of local anesthetics.
|
