Hasil Pencarian (49)
A neurotransmitter. Acetylcholine in vertebrates is the major transmitter at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. It is gen…
Amifampridine, or 3,4-diaminopyridine (3,4-DAP), is a quaternary ammonium compound that blocks presynaptic potassium channels, and subsequently prolongs the action potential and increases presynaptic calcium concentrations [A33863]. It was first discovered in…
An alkaloid obtained from the betel nut (Areca catechu), fruit of a palm tree. It is an agonist at both muscarinic and nicotinic acetylcholine receptors. It is used in the form of various salts as a ganglionic stimulant, a parasympathomimetic, and a vermifuge…
Atropine is an alkaloid originally synthesized from Atropa belladonna. It is a racemic mixture of d-and l-hyoscyamine, of which only l-hyoscyamine is pharmacologically active.[A251670,L42835] Atropine is generally available as a sulfate salt and can be admini…
Bethanechol is a synthetic ester that was initially synthesized in 1935.[A232905,L32539] As a cholinergic agent, bethanechol is similar in structure and pharmacological function to acetylcholine and is used in specific cases when stimulation of the parasympat…
Bupropion (also known as the brand name product Wellbutrin®) is a norepinephrine/dopamine-reuptake inhibitor (NDRI) used most commonly for the management of Major Depressive Disorder (MDD), Seasonal Affective Disorder (SAD), and as an aid for smoking cessatio…
Cevimeline is a parasympathomimetic agent that act as an agonist at the muscarinic acetylcholine receptors M1 and M3. It is indicated by the Food and Drug Administration for the treatment of dry mouth associated with Sjögren's syndrome.
A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
Cisatracurium is a non-depolarising neuromuscular blocking agent of the benzylisoquinolinium class, available in its salt form, cisatracurium besylate.[A243416,A253592] Cisatracurium has an intermediate duration of action and is one of the most commonly used …
Clidinium is a synthetic anticholinergic agent which has been shown in experimental and clinical studies to have a pronounced antispasmodic and antisecretory effect on the gastrointestinal tract. It inhibits muscarinic actions of acetylcholine at postganglion…
Cyclic guanosine monophosphate (Cyclic GMP) is a guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger…
Cycrimine is a drug used to reduce levels of acetylcholine to return a balance with dopamine in the treatment and management of Parkinson's disease.
Cytisine is an alkaloid naturally derived from the Fabaceae family of plants including the genera Laburnum and Cytisus. Recent studies have shown it to be a more effective and significantly more affordable smoking cessation treatment than nicotine replacement…
Darifenacin (Enablex®, Novartis) is a medication used to treat urinary incontinence. Darifenacin blocks M3 muscarinic acetylcholine receptors, which mediate bladder muscle contractions. This block reduces the urgency to urinate and so it should not be used…
DaxibotulinumtoxinA is an acetylcholine release inhibitor and neuromuscular blocking agent. It is a botulinum toxin without accessory proteins purified from the bacterium _Clostridium botulinum_ type A,[L47840] the gram-positive anaerobic bacterium primarily …
Decamethonium is used in anesthesia to cause paralysis. It is a short acting depolarizing muscle relaxant. It is similar to acetylcholine and acts as a partial agonist of the nicotinic acetylcholine receptor.
Demecarium is an indirect-acting parasympathomimetic agent that is used to treat glaucoma. It is a cholinesterase inhibitor or an anticholinesterase. Cholinesterase inhibitors prolong the effect of acetylcholine, which is released at the neuroeffector junctio…
Diphenhydramine - perhaps known most commonly as its brand name formulation Benadryl - is a first-generation H1 receptor antihistamine that is used extensively for the treatment of seasonal allergies, insect bites and stings, and rashes [L5263, L5266, L5269, …
In 2016, the global burden of dementia was estimated to be 43.8 million, demonstrating a significant increase from a global prevalence of 20.2 million in 1990.[A182411] Donepezil, also known as Aricept, is a piperidine derivative acetylcholinesterase inhibito…
Myasthenia gravis (MG) is an autoimmune disorder characterized by significant muscle weakness - particularly in the eye, throat, and extremities - caused by autoantibodies attacking the neuromuscular junction.[A243759] The production of IgG autoantibodies aga…
Galantamine is a tertiary alkaloid and reversible, competitive inhibitor of the acetylcholinesterase (AChE) enzyme, which is a widely studied therapeutic target used in the treatment of Alzheimer's disease.[A1018] First characterized in the early 1950s, galan…
Ganstigmine is an orally active, geneserine derived, carbamate-based acetylcholinesterase inhibitor developed for the treatment of Alzheimer's disease.
GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. Athenagen licensed the exc…
Hexocyclium is a muscarinic acetylcholine receptor antagonist which was presumably used in the treatment of gastric ulcer or diarrhea. It was once available under the tradename Tral marketed by Abbvie Inc. but has been discontinued. Proton pump inhibitors lik…
Homatropine is an anticholinergic drug that acts as an antagonist at muscarinic acetylcholine receptors. It is present in antitussives, under the trade name Hycodan, in combination with hydrocodone (dihydrocodeinone) bitartrate indicated for the symptomatic r…
Homatropine methylbromide is a quaternary ammonium muscarinic acetylcholine receptor antagonist belonging to the group of medicines called anti-muscarinics. Homatropine is used to treat duodenal or stomach ulcers or intestine problems. It can be used together…
Huperzine B is a novel acetylcholinesterase inhibitor.
Itopride is a dopamine D2 antagonist with acetylcholinesterase inhibitory actions.
Asthma is a complex condition associated with phenomena such as airway hyperresponsiveness (AHR), in which the smooth muscle in the airways (ASM) excessively contracts in response to stimuli, reducing pulmonary function and causing symptoms such as difficulty…
Metrifonate or trichlorfon is an irreversible organophosphate acetylcholinesterase inhibitor. It is a prodrug which is activated non-enzymatically into 2,2-dichlorovinyl dimethyl phosphate.
Mimopezil is an acetylcholinesterase (AChE) inhibitor that has demonstrated potential use in the treatment of Alzheimer's disease. Mimopezil is a pro-drug that is rapidly absorbed and converted into huperzine A.
Mivacurium is a bisbenzylisoquinolinium based neuromuscular blocker or muscle relaxant. It binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission.
Phenserine is under development by Axonyx, a US biopharmaceutical company that focuses on treatments for dementia. Phenserine is a next generation acetylcholinesterase (AChE) inhibitor indicated for the treatment of AD. Unlike currently marketed AChE inhibito…
A naturally occurring alkaloid derived from the _Pilocarpus_ plants, pilocarpine is a muscarinic acetylcholine agonist.[A262016, A262036] Pilocarpine is associated with parasympathomimetic effects by selectively working on muscarinic receptors.[A262036] Piloc…
ABT-089 is a neuronal nicotinic acetylcholine receptor agonist that may have therapeutic utility for the treatment of several neurological disorders including Alzheimer, Attention Deficit Hyperactivity Disorder and Schizophrenia/Schizoaffective disorders. In …
Pralidoxime is an antidote to organophosphate pesticides and chemicals. Organophosphates bind to the esteratic site of acetylcholinesterase, which results initially in reversible inactivation of the enzyme. If given within 24 hours,after organophosphate expos…
Myasthenia gravis is an autoimmune disease involving dysfunction at the neuromuscular junction, most commonly due to autoantibodies directed against the acetylcholine receptor (AChR), which results in muscle tone loss, muscle weakness, and fatigue.[A231004] A…
Rivanicline (TC-2403, RJR-2403, (E)-metanicotine) is a partial agonist at neuronal nicotinic acetylcholine receptors, binding primarily to the ?4?2 subtype. It was originally developed as a potential treatment for Alzheimer's disease for its nootropic effects…
Rivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type. Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.
Rozanolixizumab is a humanized high-affinity anti-human neonatal Fc receptor (FcRn) monoclonal antibody (IgG4P) targeting the immunoglobulin G (IgG). Rozonolixizumab itself is an IgG4P, an inactive isotype, to reduce the likelihood of unwanted chain exchange.…
Scopolamine is a tropane alkaloid isolated from members of the _Solanaceae_ family of plants, similar to [atropine] and [hyoscyamine], all of which structurally mimic the natural neurotransmitter [acetylcholine].[A228423, A228763] Scopolamine was first synthe…
Succinylcholine is a depolarizing skeletal muscle relaxant consisting of two molecules of the endogenous neurotransmitter [acetylcholine] (ACh) linked by their acetyl groups.[A19054] It has been widely used for over 50 years,[A299] most commonly in its chlori…
Tetraethylammonium is an experimental drug with no approved indication or marketed formulation. The only marketed drug containing tetraethylammonium was a combination drug called Fosglutamina B6, but this drug has now been discontinued. As an experimental age…
TOL2 is a modified form of the acetylcholine receptor being investigated for the treatment of myasthenia gravis.[A260117]
Tropicamide is an alkaloid atropine?derived anticholinergic drug and a non?selective antagonist of muscarinic acetylcholine (mACh) receptors.[A230103] Usually available in ophthalmic formulations, tropicamide is used to cause mydriasis and cycloplegia for eye…
Umeclidinium is a long-acting muscarinic antagonist (LAMA) used as a maintenance treatment for symptoms of chronic obstructive pulmonary disease (COPD). COPD is a progressive obstructive lung disease characterized by shortness of breath, cough, sputum product…
Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine recep…
Schizophrenia is a complex disease involving a number of different neurotransmitters, including serotonin, dopamine, and acetylcholine.[A264509] Positive symptoms (e.g. hallucinations, delusions) have traditionally been attributed to increased dopaminergic ac…
Zanapezil (TAK-147) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment.