nicotinic acetylcholine receptor

(noun)

A pentamer of protein subunits with two binding sites for acetylcholine which, when bound, alter the receptor's configuration and cause an internal pore to open.

Related Terms

  • Ionotropic receptors
  • metabotropic receptors
  • synaptic cleft
  • axon
  • presynaptic neuron
  • excitation-contraction coupling
  • voltage-dependent calcium channels
  • G protein-coupled receptor
  • receptor
  • electrochemical gradient
  • ionotropic receptor

(noun)

These are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons and on the postsynaptic side of the neuromuscular junction.

Related Terms

  • Ionotropic receptors
  • metabotropic receptors
  • synaptic cleft
  • axon
  • presynaptic neuron
  • excitation-contraction coupling
  • voltage-dependent calcium channels
  • G protein-coupled receptor
  • receptor
  • electrochemical gradient
  • ionotropic receptor

Examples of nicotinic acetylcholine receptor in the following topics:

  • Agonists, Antagonists, and Drugs

    • A nicotinic agonist is a drug that mimics, in one way or another, the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs).
    • Nicotinic acetylcholine receptors are receptors found in the central nervous system, the peripheral nervous systems, and skeletal muscles.
    • The development of nicotinic acetylcholine receptor agonists began in the early 1990's after the discovery of nicotine's positive effects on animal memory.
    • The nicotinic acetylcholine receptor agonist are gaining increasing attention as drug candidates for multiple central nervous system disorders such as Alzheimer's disease, schizophrenia, attention-deficit hyperactivity disorder (ADHD), and nicotine addiction.
    • In 2009 there were at least five drugs on the market that affect the nicotinic acetylcholine receptors.
  • Peripheral Motor Endings

    • Acetylcholine diffuses into the synaptic cleft and binds to the nicotinic acetylcholine receptors located on the motor end plate.
    • The depolarization activates L-type, voltage-dependent calcium channels (dihydropyridine receptors) in the T-tubule membrane, which are in close proximity to calcium-release channels (ryanodine receptors) in the adjacent sarcoplasmic reticulum.
    • Clinical Example: Myasthenia gravis is an autoimmune disorder in which circulating antibodies block the nicotinic acetylcholine receptors on the motor end plate of the neuromuscular junction.
    • This blockage of acetylcholine receptors causes muscle weakness, often first exhibiting drooping eyelids and expanding to include overall muscle weakness and fatigue.
    • Detailed view of a neuromuscular junction: 1) Presynaptic terminal; 2) Sarcolemma; 3) Synaptic vesicle; 4) Nicotinic acetylcholine receptor; 5) Mitochondrion.
  • Parasympathetic Responses

    • The ACh acts on two types of receptors, the muscarinic and nicotinic cholinergic receptors.
    • When stimulated, the preganglionic nerve releases ACh at the ganglion, which acts on nicotinic receptors of postganglionic neurons.
    • The postganglionic nerve then releases ACh to stimulate the muscarinic receptors of the target organ.
    • Two different subtypes of nicotinic acetylcholine receptors with alpha and beta subunits.
    • Acetylcholine binding sites are indicated.
  • Ionotropic and Metabotropic Receptors

    • Although both ionotropic and metabotropic receptors are activated by neurotransmitters, ionotropic receptors are channel-linked while metabotropic receptors initiate a cascade of molecules via G-proteins.
    • Two types of membrane-bound receptors are activated with the binding of neurotransmitters: ligand-gated ion channels (LGICs) inotropic receptors and metabotropic G- protein coupled receptors.
    • The prototypic ligand-gated ion channel is the nicotinic acetylcholine receptor .
    • It consists of a pentamer of protein subunits with two binding sites for acetylcholine which, when bound, alter the receptor's configuration and cause an internal pore to open.
    • Examples of metabotropic receptors include glutamate receptors, muscarinic acetylcholine receptors, GABAB receptors, most serotonin receptors, and receptors for norepinephrine, epinephrine, histamine, dopamine, neuropeptides, and endocannabinoids.
  • Cholinergic Neurons and Receptors

    • When acetylcholine binds to acetylcholine receptors on skeletal muscle fibers, it opens ligand-gated sodium channels in the cell membrane.
    • Although acetylcholine induces contraction of skeletal muscle, it acts via a different type of receptor (muscarinic, see ) to inhibit contraction of cardiac muscle fibers.
    • At the same time, acetylcholine acts through nicotinic receptors to excite certain groups of inhibitory interneurons in the cortex, which further dampen cortical activity.
    • The result was also found in Alzheimer's disease patients and smokers after nicotine (an ACh agonist) consumption.
    • This human M2 muscarinic acetylcholine receptor is bound to an antagonist
  • Neurotransmitters

    • The cholinergic system has two types of receptors: the nicotinic receptor and the acetylcholine receptor, which is known as the muscarinic receptor.
    • Both of these receptors are named for chemicals that interact with the receptor in addition to the neurotransmitter acetylcholine.
    • Nicotine, the chemical in tobacco, binds to the nicotinic receptor and activates it similarly to acetylcholine.
    • When acetylcholine binds to the nicotinic receptor, the postsynaptic cell is depolarized.
    • However, when acetylcholine binds to the muscarinic receptor, it might cause depolarization or hyperpolarization of the target cell.
  • Regulatory Proteins

    • During stimulation of the muscle cell, the motor neuron releases the neurotransmitter acetylcholine, which then binds to a post-synaptic nicotinic acetylcholine receptor.
    • A change in the receptor conformation causes an action potential, activating voltage-gated L-type calcium channels, which are present in the plasma membrane.
    • The inward flow of calcium from the L-type calcium channels activates ryanodine receptors to release calcium ions from the sarcoplasmic reticulum.
    • It is not understood whether the physical opening of the L-type calcium channels or the presence of calcium causes the ryanodine receptors to open.
  • Postganglionic Neurons

    • In the parasympathetic division, they are cholinergic and use acetylcholine as their neurotransmitter.
    • The sympathetic fibers: At the synapses within the ganglia, preganglionic neurons release acetylcholine, a neurotransmitter that activates nicotinic acetylcholine receptors on postganglionic neurons.
    • Postganglionic neurons of sweat glands release acetylcholine for the activation of muscarinic receptors.
    • The ACh acts on two types of receptors, the muscarinic and nicotinic cholinergic receptors.
    • Most transmissions occur in two stages: When stimulated, the preganglionic nerve releases ACh at the ganglion, which acts on nicotinic receptors of postganglionic neurons.
  • Function and Physiology of the Spinal Nerves

    • Nerves that release acetylcholine are said to be cholinergic.
    • In the parasympathetic system, ganglionic neurons use acetylcholine as a neurotransmitter to stimulate muscarinic receptors.
    • Instead the presynaptic neuron releases acetylcholine to act on nicotinic receptors.
    • Upper motor neurons release acetylcholine.
    • Acetylcholine is released from the axon terminal knobs of alpha motor neurons and received by postsynaptic receptors (nicotinic acetylcholine receptors) of muscles, thereby relaying the stimulus to contract muscle fibers.
  • Stimulants

    • Others block the action of certain receptors (such as the adenosine receptors) in a process known as receptor antagonism.
    • Still others cause action in other receptors (such as nicotinic acetylcholine) in a process known as receptor agonism.
    • Examples of well-known stimulants include amphetamines, MDMA, NDRIs, cocaine, caffeine, and nicotine.
    • In very low concentrations, nicotine also acts as a stimulant, and it is one of the main factors responsible for the dependence-forming properties of tobacco.
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