A channel modulator, or ion channel modulator, is a type of drug which modulates

ion channel Ion channels are pore-forming membrane proteins that allow ions to pass through the channel pore. Their functions include establishing a resting membrane potential, shaping action potentials and other electrical signals by gating the flow of ...

s. They include

channel blocker A channel blocker is the biological mechanism in which a particular molecule is used to prevent the opening of ion channels in order to produce a physiological response in a cell. Channel blocking is conducted by different types of molecules, suc ...

s and

channel opener A channel opener, also known as a channel activator, is a type of drug which facilitates ion flow through ion channels. They include the following: * Potassium channel openers * Calcium channel openers * Sodium channel openers * Chloride channel ...

Direct modulators

Ion channels are typically categorised by gating mechanism and by the ion they conduct. Note that an ion channel may overlap between different categories. Some channels conduct multiple ion currents and some are gated by multiple mechanisms. Examples of targets for modulators include: Voltage gated ion channels *

Calcium channel A calcium channel is an ion channel which shows selective permeability to calcium ions. It is sometimes synonymous with voltage-gated calcium channel, although there are also ligand-gated calcium channels. Comparison tables The following tables e ...

: see also

Calcium channel blocker Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium () through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as ...

Calcium channel opener A calcium channel opener is a type of drug which facilitates ion transmission through calcium channels. An example is Bay K8644, which is an analogue of nifedipine that specifically and directly activates L-type voltage-dependent calcium chann ...

Potassium channel Potassium channels are the most widely distributed type of ion channel found in virtually all organisms. They form potassium-selective pores that span cell membranes. Potassium channels are found in most cell types and control a wide variety of c ...

: see also

Potassium channel blocker Potassium channel blockers are agents which interfere with conduction through potassium channels. Medical uses Arrhythmia Potassium channel blockers used in the treatment of cardiac arrhythmia are classified as class III antiarrhythmic age ...

, Potassium channel opener *

Sodium channel Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's membrane. They belong to the superfamily of cation channels and can be classified according to the trigger that opens the chan ...

: see also

Sodium channel blocker Sodium channel blockers are drugs which impair the conduction of sodium ions (Na+) through sodium channels. Extracellular The following naturally-produced substances block sodium channels by binding to and occluding the extracellular pore opening ...

Sodium channel opener A sodium channel opener is a type of drug which facilitates ion transmission through sodium channels. Examples include toxins, such as aconitine, veratridine, batrachotoxin, robustoxin, palytoxin and ciguatoxins and insecticides (DDT and pyrethr ...

Chloride channel Chloride channels are a superfamily of poorly understood ion channels specific for chloride. These channels may conduct many different ions, but are named for chloride because its concentration ''in vivo'' is much higher than other anions. Several ...

: see also

Chloride channel blocker A chloride channel blocker is a type of drug which inhibits the transmission of ions (Cl−) through chloride channels. Niflumic acid is a chloride channel blocker that has been used in experimental scientific research. Another example is anthra ...

Chloride channel opener A chloride channel opener is a type of drug which facilitates ion transmission through chloride channels. An example is 1,10-phenanthroline, which activates Cystic fibrosis transmembrane conductance regulator (CFTR) chloride channels. GABA-A re ...

Transient receptor potential channel Transient receptor potential channels (TRP channels) are a group of ion channels located mostly on the plasma membrane of numerous animal cell types. Most of these are grouped into two broad groups: Group 1 includes TRPC ( "C" for canonical), TR ...

)

Ligand gated ion channel Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in res ...

s *

5-HT3 The 5-HT3 receptor belongs to the Cys-loop superfamily of ligand-gated ion channels (LGICs) and therefore differs structurally and functionally from all other 5-HT receptors (5-hydroxytryptamine, or serotonin receptors) which are G protein-coup ...

: see also

5-HT3 antagonist The 5-HT3 antagonists, informally known as "setrons", are a class of drugs that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain. With th ...

, *

GABAA receptor The GABAA receptor (GABAAR) is an ionotropic receptor and ligand-gated ion channel. Its endogenous ligand is γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Upon opening, the GABAA receptor ...

: see also GABA receptor agonist,

GABA receptor antagonist GABA receptor antagonists are drugs that inhibit the action of GABA. In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdoses of sedative drugs. Examples include bicuculline, securinine a ...

Glutamate receptor Glutamate receptors are synaptic and non synaptic receptors located primarily on the membranes of neuronal and glial cells. Glutamate (the conjugate base of glutamic acid) is abundant in the human body, but particularly in the nervous system ...

: see also

Excitatory amino acid receptor agonist An excitatory amino acid receptor agonist, or glutamate receptor agonist, is a chemical substance which agonizes one or more of the glutamate receptors. Examples include: * AMPA * Glutamic acid * Ibotenic acid * Kainic acid * ''N''-Methyl-D-asp ...

Excitatory amino acid receptor antagonist An excitatory amino acid receptor antagonist, or glutamate receptor antagonist, is a chemical substance which antagonizes one or more of the glutamate receptors. Examples include: * AP5 * Barbiturates * Dextromethorphan * Dextrorphan * Dizocilpin ...

Ionotropic glutamate receptor Ionotropic glutamate receptors (iGluRs) are ligand-gated ion channels that are activated by the neurotransmitter glutamate. They mediate the majority of excitatory synaptic transmission throughout the central nervous system and are key players in ...

Ampakine Ampakines, also stylized as AMPAkines, are a subgroup of AMPA receptor positive allosteric modulators with a benzamide or closely related chemical structure. They are also known as "CX compounds". Ampakines take their name from the AMPA receptor ...

NMDA receptor antagonist NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor ( NMDAR). They are commonly used as anesthetics for animals and humans; the state of anesthesia they induce ...

Nicotinic receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral n ...

: see also

Nicotinic agonist A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity for nicotine. Examples include nicotine (by definition), acetylcholine (the endogenous a ...

Ganglionic blocker A ganglionic blocker (or ganglioplegic) is a type of medication that inhibits transmission between preganglionic and postganglionic neurons in the autonomic nervous system, often by acting as a nicotinic receptor antagonist. Nicotinic acetylcholin ...

and

Neuromuscular-blocking drug Neuromuscular-blocking drugs block neuromuscular transmission at the neuromuscular junction, causing paralysis of the affected skeletal muscles. This is accomplished via their action on the post-synaptic acetylcholine (Nm) receptors. In cli ...

) Ion channels gated by other mechanisms (e.g. light gated and mechanosensitive ion channels). These types of channels can also be pharmacologically modulated. For lists of the substances that pharmacologically modulate them, see their respective articles.

Indirect modulators

Ion channels can also be modulated indirectly. For example with

G protein coupled receptor G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related p ...

s (GPCRs), for G protein coupled inward rectifier potassium channels (GIRKs) and M channels. Ion channels can also be modulated by

reuptake inhibitor Reuptake is the reabsorption of a neurotransmitter by a neurotransmitter transporter located along the plasma membrane of an axon terminal (i.e., the pre-synaptic neuron at a synapse) or glial cell after it has performed its function of transmi ...

s and

releasing agent A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the synapse, release of a monoamine neurotransmitter from the synapse, presynaptic neuron into the synapse, leading to an increase in the extracellular conc ...

References

Membrane transport modulators {{pharmacology-stub

Direct modulators

Indirect modulators

See also

References