muscle relaxation

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Prostaglandin E2 (PGE2) is a naturally occurring hormone involved in various physiological processes, such as smooth muscle contraction and relaxation, vasodilation and constriction, blood pressure regulation, and inflammatory regulation.

SKF96067 is a reversible gastric H+ K+-ATPase inhibitor that can induce relaxation of human airway smooth muscle in vitro.

ASM-024, a potent nicotinic receptor agonist, is a small molecule synthetic piperazine compound that promotes different targets and signaling pathways of β2-adrenergic receptors mediating smooth muscle relaxation, and is a potential compound for the treatment of asthma and chronic obstructive bronchitis with anti-inflammatory activity.

Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment.

picumeterol FA is a potent and selective β2-adrenergic receptor agonist. In in vitro and in vivo tests, picumeterol FA produces long-lasting airway smooth muscle relaxation. picumeterol FA is a pure R-enantiomer and can be used to improve lung function and reduce airway hyperresponsiveness in patients with asthma.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

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.

Isoxsuprine hydrochloride (Isolait) is a beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle.

Diphylline (Diprophylline) is a xanthine derivative. Diphylline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Diphylline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Diphylline may also antagonize adenosinereceptors. Diphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

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.

Tadalafil (IC-351) is a carboline-based compound with vasodilatory activity that selectively inhibits the cyclic guanosine monophosphate (cGMP)-specific type 5 phosphodiesterase (PDE-5), preventing cGMP degradation in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis, thereby causing prolonged muscle relaxation, vasodilation, and enhanced penile erection.

Chlorzoxazone (Chlorzoxazon) is a Muscle Relaxant. The physiologic effect of chlorzoxazone is by means of Centrally-mediated Muscle Relaxation.

Riociguat (BAY 632521) is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension.

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by its deuterium labeling.

Tiotropium bromide (BA679 BR) is a long-acting, 24 hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). Tiotropium is a muscarinic receptor antagonist, on topical application it acts mainly on M3 muscarinic receptors located in the airways to produce smooth muscle relaxation, thus producing a bronchodilatory effect.

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.

Tilozepine is a derivative of thienobenzodiazepine, exhibiting pharmacological activities including hypnosis, sedation, antipsychotic effects, and muscle relaxation.

Alfuzosin (SL 77499) is an orally available, competitive α1-adrenoceptor antagonist.Alfuzosin induces smooth muscle relaxation in the bladder neck and prostate.Alfuzosin has been used to study benign prostatic hypertrophy, lower urinary tract symptoms (LUTS), and ejaculatory dysfunction (EjD).

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.

Laudexium is a neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs. It is used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle re

Laudexium methylsulfate is a neuromuscular blocking drug or skeletal muscle relaxant. It is used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.