Ion Channels as Drug Targets

Ionic Homeostasis
Major inorganic cations and anions found in both the plasma and intracellular membranes. Used in the regulation in ionicgradients.
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Potassium Channels
Regulate cell excitability through different modalities. Involved in the frequency/shape of action potientials, secreting hormones/neurotransmitters and membrane potential.
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Minoxidil
Opens K+ channels, causes hyperpolarisation in smooth muscle cells. Treats hypertension and promotes hair growth by opening potassium channels to allow nutrients to get to the hair follicles.
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Sodium Channels
Voltage-gated sodium selective ion channels found in excitable cells with action potentials.
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Sodium Channel Pores
Attract the positive Na+ ion and keep out negatively charged ions such as chlorine. Ions of different sizes also can not interact as well with the negatively charged glutamic acid residues that line the pore.
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Lidocaine
Block voltage-gated sodium channels. Target the Nav1.5 which is the main cardiac sodium channel. Used to treat ventricular arrhythmias specially after myocardial infraction. Also a local aesthetic
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Calcium Channels
Form hetero-oligometeric complexes. 3 Families exist: high-voltage dihuropyridine-sensitive, high-voltage dihuropyridine-insensitive, low voltage activated channels. Used in a variety of processes such as muscle contractions and hormone release.
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Trans-membrane topology of the calcium channel a-sub units
Locations of mutations in Cav3.2 that have been linked to idopathic generalised epilepsy.
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Verapamil
Blocks calcium channels, in myocardial and vasular smooth muscle cells. Leads to a reduction in contraction causing dilation in coronary and systemic arteries.
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TRP Channels
Found in the plasma membrane of numerous cell types. Have: N&C terminals, heat sensitive, respond to mechanical stimuli.
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Channelopathies
Diseases caused by disturbed function of ion channel subunits. Can be congenital or acquired e.g epilepsy, diabetes or ataxia
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Ligand gated channels
Also called ionotropic receptors, link ligand binding to an ionic flux with fast synaptic transmission. e.g nitcotinic ACh receptors.
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Acetylcholine Receptors
4 transmembrane domains, TM2 from each subunit lines the ion channel pores. Na+ flows along the concentration gradient which causes depolarisation of cell e.g muscle contraction and neuron action potential
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(a1)2b1dy
Muscle subtype
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(a4)2(b2)3
CNS subtypes
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Succinylcholine
Full agonist of the nACh receptor that minics the effects of Ach, used as a neuromusclar blockage for surgery
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5-HT3 Antagonists
Class of drugs that act as receptor antagonist. Mediates synaptic transmisson to the medullary vomiting centre, Used to treat nausea and vomiting induced by cytotoxic chemotherapy.
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Diazepam
Full agonist of GABAa Receptor. Used as a short term treatment for anxiety or insomnia.
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Other cards in this set

Card 2

Front

Regulate cell excitability through different modalities. Involved in the frequency/shape of action potientials, secreting hormones/neurotransmitters and membrane potential.

Back

Potassium Channels

Card 3

Front

Opens K+ channels, causes hyperpolarisation in smooth muscle cells. Treats hypertension and promotes hair growth by opening potassium channels to allow nutrients to get to the hair follicles.

Back

Preview of the back of card 3

Card 4

Front

Voltage-gated sodium selective ion channels found in excitable cells with action potentials.

Back

Preview of the back of card 4

Card 5

Front

Attract the positive Na+ ion and keep out negatively charged ions such as chlorine. Ions of different sizes also can not interact as well with the negatively charged glutamic acid residues that line the pore.

Back

Preview of the back of card 5
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