Abstract:
:Recent controversies in the existence of saturable binding of general anesthetics in brain tissues prompted a careful examination of specific binding of anesthetics to neural receptors. We examined the binding of both local and general anesthetics using electron spin resonance and radioligand criteria. Our results suggested that the hydrophobic path, most probably through the lipid bilayer, figures importantly in the binding of the uncharged moieties of anesthetics. Competitive interactions by hydrophobic compounds for the high-affinity site in the nicotinic acetylcholine receptor led us to propose a hypothesis that includes a hydrophobic crevice of limited volume as part of the high-affinity site. Association of anesthetic at this crevice is in turn dependent on the anesthetic concentration in the lipid phase of the membrane. The hypothesis provides a mechanism for the saturable interaction of anesthetics with their protein target site in the membrane without violating the correlations expressed by the Meyer-Overton rule of anesthetic action.
journal_name
Ann N Y Acad Scijournal_title
Annals of the New York Academy of Sciencesauthors
Lin L,Koblin DD,Wang HHdoi
10.1111/j.1749-6632.1991.tb33897.xsubject
Has Abstractpub_date
1991-01-01 00:00:00pages
628-44eissn
0077-8923issn
1749-6632journal_volume
625pub_type
杂志文章,评审abstract::The elderly, often defined as those 65 years or older, are the most rapidly growing segment of the population, and onset of epilepsy is higher in this age group than in any other. This paper reviews recent developments, including a new proposed definition of epilepsy, a transgenic mouse model of Alzheimer's disease th...
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