The effect of propoxycaine.HCl on the physical properties of neuronal membranes.
Fluorescent probe techniques were used to evaluate the effect of propoxycaine.HCl on the physical properties (transbilayer asymmetric lateral and rotational mobilities, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMVs) isolated from bovine cerebral cortex. An experimental procedure was used based on selective quenching of both 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer (RET) from the tryptophans of membrane proteins to Py-3-Py. Propoxycaine.HCl increased the bulk lateral and rotational mobilities, and annular lipid fluidity in SPMVs lipid bilayers, and had a greater fluidizing effect on the inner monolayer than that of the outer monolayer. The magnitude of increasing effect on annular lipid fluidity in SPMVs lipid bilayer induced by propoxycaine.HCl was significantly far greater than magnitude of increasing effect of the drug on the lateral and rotational mobilities of SPMVs lipid bilayer. It also caused membrane proteins to cluster. These effects of propoxycaine.HCl on neuronal membranes may be responsible for some, though not all, of the local anesthetic actions of propoxycaine.HCl.
Lee
Jong-Hwa
JH
Department of Dental Pharmacology and Biophysics, College of Dentistry and Research Institute for Oral Biotechnology, Pusan National University, Busan 602-739, Republic of Korea.
Kim
Dong-Il
DI
Mun
Hun
H
Lee
Sung-Key
SK
Park
Jong-Sun
JS
Kim
Jong-Ho
JH
Lee
Jang-Hoon
JH
Park
Yi-Hoon
YH
Jeon
Young-Chan
YC
Yoon
Ung-Chan
UC
Bae
Moon-Kyung
MK
Jang
Hye-Ock
HO
Wood
W Gibson
WG
Yun
Il
I
D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D002417:Cattle; D002540:Cerebral Cortex / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004735:Energy Transfer; D005456:Fluorescent Dyes; D008560:Membrane Fluidity / Q000187:drug effects* / Q000502:physiology; D008565:Membrane Proteins / Q000737:chemistry / Q000378:metabolism*; D011430:Propoxycaine / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence; D013570:Synaptic Membranes / Q000187:drug effects* / Q000378:metabolism
D000779:Anesthetics, Local; D005456:Fluorescent Dyes; D008565:Membrane Proteins; D011430:Propoxycaine