neuromuscular

Neuromuscular-targeting compound 1 can be used to study muscular dystrophy and neuromuscular-related diseases.

Neuromuscular Disorder-Targeting Compound 1 is utilized in research for neuromuscular disorders, including chronic fatigue syndrome and fibromyalgia syndrome symptoms.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Vecuronium bromide (ORG NC 45) is a synthetic, intermediate-acting, mono-quaternary steroid that functions as a non-depolarizing neuromuscular blocking agent with muscle relaxant properties.

Decamethonium bromide (Syncurine) is a neuromuscular blocker and nicotinic AChR partial agonist.

Dantrolene sodium (Lapatinib ditosylate monohydrate) salt is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.

Amifampridine (3,4-Diaminopyridine) is primarily used to treat rare muscle diseases. It blocks potassium channel efflux in nerve terminals, increasing action potential duration, which allows Ca2+ channels to remain open longer and enhances acetylcholine release to stimulate muscles at the end plate.

Succinylcholine Chloride Dihydrate (Succinyldicholine dichloride) is a nicotinic AChR agonist and also acts as a depolarizing neuromuscular blocker.

Pancuronium dibromide (Pavulon), a competitive AChR antagonist (IC50 = 5.5 nM), acts as a skeletal muscle relaxant. Pancuronium dibromide(Pancuronium bromide) blocking neuromuscular transmission is achieved by competing with acetylcholine for receptor sites on the motor end-plate.

Acetylcholine iodide (Acetylcolina) is a neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.

Rocuronium bromide (ORG 9426) is a muscle relaxant or aminosteroid non-depolarizing neuromuscular blocker. During surgery or mechanical ventilation, it is used to facilitate endotracheal intubation and to provide skeletal muscle relaxation.

Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist. Acetamiprid is a neonicotinoid insecticide used worldwide. It is shown to be associated with neuromuscular and reproductive disorders.

Pyrantel pamoate (Pyrantel embonate) is a depolarizing neuromuscular blocking agent. This compound is commonly used as an anthelmintic to treat parasitic worm infections, effectively paralyzing nematodes by inhibiting their neuromuscular activity.

Sugammadex sodium (Org25969) , a synthetic derivative of γ-cyclodextrin, is a steroid-based neuromuscular blocker reversing agent.

Argireline (Acetyl hexapeptide-3) is a peptide composed of amino acid chains that significantly inhibits Ca2+-dependent neurotransmitter (acetylcholine) release at the neuromuscular junction, exhibiting notable anti-wrinkle and anti-aging activity[1][2][3].

1. Tuberostemonine (Tuberstemonine) exhibits relatively higher intestinal permeabilities. 2. Tuberostemonine acts in part as an open-channel blocker at the crayfish neuromuscular junction.

5,5-Dimethyloxazolidine-2,4-dione (Dimethadione) is an anticonvulsant that is the active metabolite of TRIMETHADIONE.

Proctolin is a bioactive neuropeptide that modulates interneuronal and neuromuscular synaptic transmission in a wide variety of arthropods.

NMD670 is an orally active, partial inhibitor of the skeletal muscle-specific chloride channel ClC-1. It enhances muscle excitability and neuromuscular transmission, restoring muscle function and mobility. NMD670 has a favorable safety profile and improves muscle function in rats, particularly in an MG rat model [1].

S1PL-IN-31 is a dual-function chemical compound acting as an inhibitor of sphingosine-1-phosphate (S1P) lyase with an IC50 value of 210 nM and as an antagonist of the Smoothened (Smo) receptor with an IC50 of 440 nM. Demonstrating therapeutic potential, this compound, at a dosage of 2 mg/kg per day, effectively mitigates cervical and thoracic lymphocyte infiltration and neuromuscular weakness in rats suffering from experimental autoimmune encephalomyelitis (EAE), a condition triggered by the MOG29-152 peptide from myelin oligodendrocyte glycoprotein. Additionally, it significantly decreases the total lymphocyte count, including reductions in subsets of CD4+ T cells, CD8+ T cells, and B cells. At a higher dosage of 100 mg/kg, S1PL-IN-31 elevates S1P levels within the heart and lymph nodes, while doses of 3 and 10 mg/kg per day notably lower heart rates in female rats, showcasing its multifaceted biological impacts and potential for clinical application.

Pancuronium is an aminosteroid antagonist of muscle-type nicotinic acetylcholine receptors (nAChRs) with an IC50value of 14.8 nM using patch clamp electrophysiology in BOSC23 cells expressing mouse nAChRs.1It acts as a non-depolarizing neuromuscular blocking agent.2Pancuronium enhances anesthesia induced by isoflurane , reducing immobilization with an ED50value of 1.62 μg/kg.3 1.Liu, M., and Dilger, J.P.Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholine receptorMol. Pharmacol.75(1)166-173(2009) 2.Buckett, W.R., Marjoribanks, C.E., Marwick, F.A., et al.The pharmacology of pancuronium bromide (Org.NA97), a new potent steroidal neuromuscular blocking agentBr. J. Pharmacol. Chemother.32(3)671-682(1968) 3.Miyazaki, Y., Sunaga, H., Hobo, S., et al.Pancuronium enhances isoflurane anesthesia in rats via inhibition of cerebral nicotinic acetylcholine receptorsJ. Anesth.30(4)671-676(2016)

Metocurine is a muscle relaxant through neuromuscular blockade. It is excreted entirely through the kidneys and therefore should not be used in patients with kidney failure.

Decamethonium (Syncurine) is a depolarizing muscle relaxant or neuromuscular blocking agent, and is used in anesthesia to induce paralysis.

Dacuronium is a new steroidal drug of neuromuscular blocking properties. Dacuronium produced a competitive type of neuromuscular block with a potency of approximately one-tenth that of tubocurarine and one-fiftieth that of pancuronium.

Apitegromab (SRK-015) is a new myostatin inhibitor, an antibody targeting myostatin precursor, which can be used to study neuromuscular diseases including spinal muscular atrophy.

Mivacurium dichloride (Mivacurium chloride) is a non-depolarising, rapid neuromuscular blocker of short duration, used therefore as anesthetic, to provide skeletal muscle relaxation in minor surgical operations, in emergency surgical procedures of short to intermediate duration and during intubation of the trachea.

Acetylcholine bromide is the bromide salt of acetylcholine. It is an neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central ner

Bethanidine sulfate and its ortho-chloro derivative (BW 392C60) are potent adrenergic neuron blockers exhibiting sympathomimetic effects similar to those of bromobenzamine and guanethidine in various animal models, particularly in cats. These compounds inhibit the release of norepinephrine during neural stimulation and enhance the responsiveness of smooth muscle to epinephrine and norepinephrine. Notably, bethanidine sulfate increases the pressor response to tyramine, although this effect diminishes with higher doses. Unlike guanethidine, bethanidine sulfate does not deplete pressor amines in the iris of cats following administration. Additionally, it temporarily suppresses autonomic cholinergic mechanisms and can cause transient neuromuscular paralysis at large doses, contrasting its long-term adrenergic neuron blocking effects.

Stilbamidine dihydrochloride is a blocker of neuromuscular transmission and axonal conduction used to study the distribution of the drug in the organs and tissues of rats following intravenous injection.

Lophotoxin belongs to the cembrene class of diterpenoids; neuromuscular toxin isolated from several pacific gorgonians of the genus Lophogorgia.

Ambenonium chloride tetrahydrate is a salt of ambenonium --- a quaternary ammonium compound with parasympathomimetic activity. It is a cholinesterase inhibitor used in the management of myasthenia gravis. Myasthenia gravis occurs when the body produces antibodies against acetylcholine receptors, and thus inhibits signal transmission across the myoneural junction. Ambenonium chloride is a rapid indirect-acting cholinergic agonist that reversibly blocks the activity of acetylcholinesterase, thereby prevents acetylcholine hydrolysis and prolonging its activity on nicotinic receptors at the neuromuscular junction.

Norcoralydine is a neuromuscular blocking agent.

Atracurium (BW-33A free acid) is a potent, competitive, non-depolarizing neuromuscular blocking agent and AChR receptor antagonist that induces bronchoconstriction and neuromuscular blockade, while also promoting astroglial differentiation [1] [2] [3] [4] [5].

α-CGRP, rat TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies [1] [2] [3] .

Botulinum toxin type B, an antigen-specific exotoxin produced by the anaerobic bacterium Clostridium botulinum, is utilized in the study of neck dystonia. It inhibits the release of Acetylcholine from the neuromuscular junction, causing relaxation paralysis or muscle weakening in the targeted muscle [1].

CGP 35348 is a selective antagonist of GABAB receptor (EC50 = 34 μM). CGP 35348 can be used in studies of neuromuscular coordination and spatial learning after neonatal brain damage in albino mice.

Selective antagonist of neuromuscular nicotinic receptors α1β1γδ

Rocuronium is an blocker of aminosteroid non-depolarizing neuromuscular.

Pipecuronium bromide (RGH-1106) is a selective and potent nAChR antagonist that also acts as a non-depolarising steroidal neuromuscular blocker, causing muscle relaxation, often in conjunction with antibiotics.

3- Deoxyaconitine is a derivative of Aconitine (A189875), which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction.

αC-Conotoxin PrXA is a neurotoxic paralytic peptide acting as a competitive antagonist of the nicotinic acetylcholine receptor (nAChR), exhibiting inhibitory constants (IC50) of 1.8 nM for the adult α1β1εδ subtype and 3.0 nM for the fetal α1β1γδ subtype. The compound vies with α-bungarotoxin for binding sites at the α/δ and α/γ interfaces of neuromuscular nAChRs, demonstrating high selectivity[1].

Monarsen (EN101), a synthetic 20-base antisense oligodeoxynucleotide targeting the human AChE gene, is utilized in researching autoimmune myasthenia gravis (MG). This neuromuscular disorder is characterized by autoantibodies targeting the acetylcholine receptor (AChR).

Tirasemtiv (CK-2017357)(CK 2017357) is a small-molecule fast-skeletal-troponin activator, with a potential treatment for muscle weakness and neuromuscular dysfunction.

Oxybutynin R-isomer , also known as Aroxybutynin, is a muscarinic receptor antagonist. Aroxybutynin is the optically avtice inhibitor of proliferation and supresses gene expression in bladder smooth muscle cells. Oxybutynin exerts direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. It exhibits one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects).

Astromicin Sulfate is an antibiotic with aminoglycoside structure. Astromicin Sulfate may produce depression of neuromuscular function.

Decamethonium is a depolarizing muscle relaxant or neuromuscular blocking agent,[1] and is used in anesthesia to induce paralysis.

Ambenonium Chloride is the chloride salt form of ambenonium, a quaternary ammonium compound with parasympathomimetic activity. It is a cholinesterase inhibitor used in the management of myasthenia gravis. Myasthenia gravis occurs when the body produces antibodies against acetylcholine receptors, and thus inhibits signal transmission across the myoneural junction. Ambenonium chloride is a rapid indirect-acting cholinergic agonist that reversibly blocks the activity of acetylcholinesterase, thereby prevents acetylcholine hydrolysis and prolonging its activity on nicotinic receptors at the neuromuscular junction.