TRENDS in Neurosciences Vol.24 No.6 June 2001
http://tins.trends.com
339 Review Review Review
Leak or background K
+
selective channels – defined
by a lack of voltage- and time-dependency, and with a
linear current to voltage relationship in a
symmetrical K
+
gradient – play an essential role in
setting the resting membrane potential, tuning the
action potential duration and modulating the
responsiveness to synaptic inputs. Regulation of
background K
+
channels by neurotransmitters and
second messengers is central for synaptic function
1,2
.
The most extensively studied native background K
+
channel is the S channel in the marine snail Aplysia
sensory neurones
1
. Closing of the S-type background
K
+
channel by 5-HT receptor activation is involved in
presynaptic sensitization, a simple form of learning
2
.
Additionally, neuronal background K
+
channels are
the targets of an important class of pharmacological
agents, the volatile general anaesthetics
3–7
.
Mammalian K
+
channel subunits (~80 genes) can
be divided into three main structural classes
comprising two transmembrane segments (TMS),
four-TMS or six-TMS (Ref. 8). The common feature of
all K
+
channels is the presence of a conserved motif
called the P domain, which is part of the K
+
conduction pathway
9
. The two-TMS channels
comprise a single P domain and encode the inward
rectifiers. These K
+
channels, which operate at
negative membrane potentials, contribute to the
setting of the resting membrane potential. The six-
TMS channels, including the voltage-gated and the
Ca
2+
-activated K
+
channels, similarly comprise a
single P domain. These channels, which are usually
activated at depolarized membrane potentials, mostly
contribute to the repolarization of the action
potential. By contrast, the most recently discovered
class of four-TMS subunits is characterized by the
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Review
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Review
Properties and modulation of
mammalian 2P domain K
+
channels
Amanda J. Patel and Eric Honoré
Mammalian 2P domain K
+
channels are responsible for background or ‘leak’ K
+
currents.These channels are regulated by various physical and chemical
stimuli, including membrane stretch, temperature, acidosis, lipids and
inhalational anaesthetics. Furthermore, channel activity is tightly controlled by
membrane receptor stimulation and second messenger phosphorylation
pathways.Several members of this novel family of K
+
channels are highly
expressed in the central and peripheral nervous systems in which they are
proposed to play an important physiological role.The pharmacological
modulation of this novel class of ion channels could be of interest for both
general anaesthesia and ischaemic neuroprotection.
Amanda J. Patel
Eric Honoré*
Institut de Pharmacologie
Moléculaire et Cellulaire,
CNRS-UMR6097, 660
route des Lucioles,
Sophia Antipolis, 06560
Valbonne, France.
*e-mail: honore@
ipmc.cnrs.fr