Nicotinic acetylcholine receptor in the context of Neuromuscular blocking agent


Nicotinic acetylcholine receptor in the context of Neuromuscular blocking agent

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⭐ Core Definition: Nicotinic acetylcholine 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 nervous system, muscle, and many other tissues of many organisms. At the neuromuscular junction they are the primary receptor in muscle for motor nerve-muscle communication that controls muscle contraction. In the peripheral nervous system: (1) they transmit outgoing signals from the presynaptic to the postsynaptic cells within the sympathetic and parasympathetic nervous system; and (2) they are the receptors found on skeletal muscle that receives acetylcholine released to signal for muscular contraction. In the immune system, nAChRs regulate inflammatory processes and signal through distinct intracellular pathways. In insects, the cholinergic system is limited to the central nervous system.

The nicotinic receptors are considered cholinergic receptors, because they respond to acetylcholine. Nicotinic receptors get their name from nicotine, which selectively binds to nicotinic receptors but not to other acetylcholine receptors. (The other type of acetylcholine receptor, the muscarinic receptor, likewise gets its name from a chemical that selectively attaches to that receptor: muscarine. Acetylcholine itself binds to both muscarinic and nicotinic acetylcholine receptors.)

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👉 Nicotinic acetylcholine receptor in the context of Neuromuscular blocking agent

Neuromuscular-blocking drugs, or Neuromuscular blocking agents (NMBAs), block 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 clinical use, neuromuscular block is used adjunctively to anesthesia to produce paralysis, firstly to paralyze the vocal cords, and permit endotracheal intubation, and secondly to optimize the surgical field by inhibiting spontaneous ventilation, and causing relaxation of skeletal muscles. Because the appropriate dose of neuromuscular-blocking drug may paralyze muscles required for breathing (i.e., the diaphragm), mechanical ventilation should be available to maintain adequate respiration.

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Nicotinic acetylcholine receptor in the context of Smoking

Smoking is a human behavior which involves the combustion of a substance, usually plant material, and the inhalation of resulting fumes. Today smoking is mostly practiced by rolling the dried leaves of the tobacco plant into a cigarette. Other forms of tobacco smoking include the use of a smoking tobacco with a pipe or cigar, or using a bong. Cigarette smokers almost always inhale the smoke; most pipe and cigar smokers do not inhale.

Smoking is primarily practiced as a route of administration for psychoactive chemicals because the active substances within the burnt, dried plant leaves (or other chemical) can vaporize into a gaseous state and be delivered into the respiratory tract, where they are rapidly absorbed into the bloodstream through the lungs and can reach the central nervous system. In the case of tobacco smoking, these active substances are a mixture of aerosol particles that include the pharmacologically active alkaloid nicotine, which stimulates the nicotinic acetylcholine receptors in the brain, and other non-psychoactive chemicals that result from combustion. Other notable drugs inhaled via smoking include tetrahydrocannabinol (from cannabis), morphine (from opium) cocaine (from crack), and methamphetamine. Designer drugs, or "research chemicals", can also be smoked.

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Nicotinic acetylcholine receptor in the context of Receptor (biochemistry)

In biochemistry and pharmacology, receptors are chemical structures, composed of protein, that receive and transduce signals that may be integrated into biological systems. These signals are typically chemical messengers which bind to a receptor and produce physiological responses, such as a change in the electrical activity of a cell. For example, GABA, an inhibitory neurotransmitter, inhibits electrical activity of neurons by binding to GABAA receptors. There are three main ways the action of the receptor can be classified: relay of signal, amplification, or integration. Relaying sends the signal onward, amplification increases the effect of a single ligand, and integration allows the signal to be incorporated into another biochemical pathway.

Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. A molecule that binds to a receptor is called a ligand and can be a protein, peptide (short protein), or another small molecule, such as a neurotransmitter, hormone, pharmaceutical drug, toxin, calcium ion or parts of the outside of a virus or microbe. An endogenously produced substance that binds to a particular receptor is referred to as its endogenous ligand. E.g. the endogenous ligand for the nicotinic acetylcholine receptor is acetylcholine, but it can also be activated by nicotine and blocked by curare. Receptors of a particular type are linked to specific cellular biochemical pathways that correspond to the signal. While numerous receptors are found in most cells, each receptor will only bind with ligands of a particular structure. This has been analogously compared to how locks will only accept specifically shaped keys. When a ligand binds to a corresponding receptor, it activates or inhibits the receptor's associated biochemical pathway, which may also be highly specialised.

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Nicotinic acetylcholine receptor in the context of Nicotine

Nicotine is an alkaloid found primarily in plants of the nightshade family, notably in tobacco and Duboisia hopwoodii. In addition to extraction from tobacco, it is synthesized. Nicotine is used recreationally for its stimulant and anxiolytic effects. In tobacco leaves, nicotine constitutes about 0.6–3.0% of the dry weight, and smaller, trace quantities occur in other Solanaceae crops such as tomatoes, potatoes, and eggplants. In pure form, nicotine is a colorless to yellowish, oily liquid that readily penetrates biological membranes and acts as a potent neurotoxin in insects, where it serves as a antiherbivore toxin. Historically, it was widely used as an insecticide, and its structure provided the basis for synthetic neonicotinoid pesticides.

In humans, nicotine acts primarily as a stimulant by binding to and activating nicotinic acetylcholine receptors (nAChRs) in the central nervous system and peripheral tissues. This results in the release of neurotransmitters such as dopamine, acetylcholine, and norepinephrine, producing effects including increased alertness, reduced anxiety, and mild euphoria. Nicotine is typically consumed through tobacco smoking, vaping, or other nicotine delivery systems. An average cigarette yields about 2 mg of absorbed nicotine, a dose sufficient to produce reinforcement and dependence while remaining far below toxic levels.

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Nicotinic acetylcholine receptor in the context of Myasthenia gravis

Myasthenia gravis (MG) is a long-term neuromuscular junction disease that leads to varying degrees of skeletal muscle weakness. The most commonly affected muscles are those of the eyes, face, and swallowing. It can result in double vision, drooping eyelids, and difficulties in talking and walking. Onset can be sudden. Those affected often have a large thymus or develop a thymoma.

Myasthenia gravis is an autoimmune disease of the neuromuscular junction which results from antibodies that block or destroy nicotinic acetylcholine receptors (AChR) at the junction between the nerve and muscle. This prevents nerve impulses from triggering muscle contractions. Most cases are due to immunoglobulin G1 (IgG1) and IgG3 antibodies that attack AChR in the postsynaptic membrane, causing complement-mediated damage and muscle weakness. Rarely, an inherited genetic defect in the neuromuscular junction results in a similar condition known as congenital myasthenia. Babies of mothers with myasthenia may have symptoms during their first few months of life, known as neonatal myasthenia or more specifically transient neonatal myasthenia gravis. Diagnosis can be supported by blood tests for specific antibodies, the edrophonium test, electromyography (EMG), or a nerve conduction study.

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Nicotinic acetylcholine receptor in the context of Autoimmune autonomic ganglionopathy

Autoimmune autonomic ganglionopathy is a type of immune-mediated autonomic failure that is associated with antibodies against the ganglionic nicotinic acetylcholine receptor present in sympathetic, parasympathetic, and enteric ganglia. Typical symptoms include gastrointestinal dysmotility, orthostatic hypotension, and tonic pupils. Many cases have a sudden onset, but others worsen over time, resembling degenerative forms of autonomic dysfunction. For milder cases, supportive treatment is used to manage symptoms. Plasma exchange, intravenous immunoglobulin, corticosteroids, or immunosuppression have been used successfully to treat more severe cases.

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Nicotinic acetylcholine receptor in the context of Cholinomimetic

A parasympathomimetic drug, sometimes called a cholinomimetic drug or cholinergic receptor stimulating agent, is a substance that stimulates the parasympathetic nervous system (PSNS). These chemicals are also called cholinergic drugs because acetylcholine (ACh) is the neurotransmitter used by the PSNS. Chemicals in this family can act either directly by stimulating the nicotinic or muscarinic receptors (thus mimicking acetylcholine), or indirectly by inhibiting cholinesterase, promoting acetylcholine release, or other mechanisms. Common uses of parasympathomimetics include glaucoma, Sjögren syndrome and underactive bladder.

Some chemical weapons such as sarin or VX, non-lethal riot control agents such as tear gas, and insecticides such as diazinon fall into this category.

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